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ChEMBL ligand: CHEMBL370805 (Benzoylmethylecgonine, Cocaine, Cocainum, IDS-NC-004, Neurocaine, (r)-(-)-cocaine, RX-0041, RX0041) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Dopamine transporter in Macaca fascicularis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5032] [UniProtKB: Q9GJT6] | ||||||||
ChEMBL | Inhibition of [3H]WIN-35428 binding to dopamine transporter (DAT) of cynomolgus monkey caudate-putamen | B | 7.02 | pIC50 | 95.6 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 857-862 [PMID:10206550] |
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
ChEMBL | Inhibition of [3H]mazindol binding to recombinant human DAT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis | B | 5.9 | pKi | 1270 | nM | Ki | J Med Chem (2017) 60: 3109-3123 [PMID:28319392] |
ChEMBL | Inhibition of [125I]RTI-55 binding to dopamine transporter | B | 6.12 | pKi | 760 | nM | Ki | J Med Chem (2000) 43: 205-213 [PMID:10649976] |
ChEMBL | Inhibition of [125I]RTI-55 binding at Dopamine transporter (DAT) expressed in HEK cells | B | 6.12 | pKi | 759 | nM | Ki | J Med Chem (1999) 42: 3647-3656 [PMID:10479296] |
ChEMBL | Inhibition of [125I]RTI-55 binding to recombinant human DAT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis | B | 6.14 | pKi | 720 | nM | Ki | J Med Chem (2017) 60: 3109-3123 [PMID:28319392] |
ChEMBL | Displacement of [125I]RTI55 from human DAT expressed in COS1 cell membrane | B | 6.2 | pKi | 630 | nM | Ki | Bioorg Med Chem (2007) 15: 4159-4174 [PMID:17446076] |
ChEMBL | Displacement of [125I]RTI-55 from human DAT expressing HEK293 cells | B | 6.3 | pKi | 500 | nM | Ki | J Med Chem (2007) 50: 219-232 [PMID:17228864] |
ChEMBL | Displacement of [125I]- RTI-55 from Dopamine transporter expressed in HEK cells | B | 6.31 | pKi | 490 | nM | Ki | J Med Chem (2002) 45: 4097-4109 [PMID:12213053] |
ChEMBL | Displacement of [3H]WIN 35428 from human DAT transiently expressed in COS7 cells | B | 6.35 | pKi | 450 | nM | Ki | J Med Chem (2020) 63: 2343-2357 [PMID:31661268] |
ChEMBL | Displacement of [125I]RTI-55 from human DAT expressed in HEK293 cells | B | 6.36 | pKi | 432 | nM | Ki | J Med Chem (2006) 49: 1420-1432 [PMID:16480278] |
ChEMBL | Displacement of [125I]RTI-55 from human recombinant DAT expressed in HEK293 cells | B | 6.37 | pKi | 431 | nM | Ki | Bioorg Med Chem (2009) 17: 6890-6897 [PMID:19740668] |
ChEMBL | Displacement of [125I]RT155 binding in HEK cells expressing human DAT | B | 6.38 | pKi | 419 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 4133-4137 [PMID:14592523] |
ChEMBL | Binding affinity towards dopamine transporter using [3H]WIN-35428 as radioligand from rat caudate putamen tissue (low affinity) | B | 6.41 | pKi | 388 | nM | Ki | J Med Chem (1996) 39: 1560-1563 [PMID:8691489] |
ChEMBL | Displacement of [125I]RTI55 from human recombinant DAT expressed in HEK293 cells | B | 6.43 | pKi | 371 | nM | Ki | Bioorg Med Chem (2009) 17: 337-343 [PMID:19014888] |
ChEMBL | Displacement of [125I]RTI55 from human DAT expressed in HEK cells | B | 6.43 | pKi | 371 | nM | Ki | Bioorg Med Chem (2009) 17: 2047-2068 [PMID:19201198] |
ChEMBL | Displacement of [125I]RTI-55 from human recombinant DAT expressed in HEK293 cells by scintillation counting | B | 6.43 | pKi | 371 | nM | Ki | J Med Chem (2009) 52: 1530-1539 [PMID:19256502] |
ChEMBL | Inhibition of [3H]DA uptake in human DAT expressed in COS1 cell membrane | F | 6.46 | pKi | 347 | nM | Ki | Bioorg Med Chem (2007) 15: 4159-4174 [PMID:17446076] |
ChEMBL | Binding affinity at DAT | B | 6.47 | pKi | 341 | nM | Ki | J Med Chem (2008) 51: 2795-2806 [PMID:18393401] |
ChEMBL | Inhibition of reuptake of [3H]DA (20 nM) by dopamine transporter | B | 6.48 | pKi | 330 | nM | Ki | J Med Chem (2000) 43: 4981-4992 [PMID:11150168] |
ChEMBL | Binding affinity against cloned human dopamine transporter using 40-80 pM [125I]RTI. | B | 6.52 | pKi | 300 | nM | Ki | J Med Chem (2000) 43: 4981-4992 [PMID:11150168] |
ChEMBL | Compound was evaluated for inhibition of [3H]DA uptake in HEK-hDAT cells expressing Human dopamine Transporter | B | 6.56 | pKi | 276 | nM | Ki | J Med Chem (2000) 43: 2064-2071 [PMID:10821718] |
ChEMBL | Compound was tested for inhibition of [125I]RTI-55 binding to dopamine transporter in HEK cells | B | 6.57 | pKi | 272 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2151-2154 [PMID:12798324] |
ChEMBL | Displacement of [125I]RTI55 from cloned human DAT expressed in HEK293 cells | B | 6.57 | pKi | 272 | nM | Ki | J Med Chem (2009) 52: 6768-6781 [PMID:19821577] |
ChEMBL | Affinity to inhibit [3H]DA uptake | B | 6.57 | pKi | 270 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 513-517 [PMID:12565962] |
ChEMBL | Compound was evaluated for binding affinity to dopamine transporter using [125I]RTI-55 as a radioligand in HEK cells expressing human transporters. | B | 6.59 | pKi | 258 | nM | Ki | J Med Chem (2000) 43: 2064-2071 [PMID:10821718] |
ChEMBL | Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay | B | 6.6 | pKi | 249 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445] |
ChEMBL | Ability of compound to inhibit dopamine uptake of receptor was determined | B | 6.63 | pKi | 234.42 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2149-2157 [PMID:15808487] |
ChEMBL | Binding Affinity to Dopamine transporter in caudate nuclei which was homogenized and incubated with [3H]mazindol. | B | 6.64 | pKi | 231 | nM | Ki | J Med Chem (2000) 43: 351-360 [PMID:10669562] |
ChEMBL | Displacement of [3H]WIN35,428 from wild type human DAT expressed in COS7 cell membranes incubated for >90 mins by radioligand binding assay | B | 6.65 | pKi | 223 | nM | Ki | J Med Chem (2016) 59: 10676-10691 [PMID:27933960] |
ChEMBL | Inhibition of DAT (unknown origin) expressed in COS7 cells assessed as reduction in [3H]DA uptake incubated for 5 mins by beta-scintillation counting method | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (2016) 59: 10676-10691 [PMID:27933960] |
ChEMBL | Binding affinity towards dopamine transporter using [3H]WIN-35428 as radioligand from rat caudate putamen tissue (high affinity) | B | 7.49 | pKi | 32 | nM | Ki | J Med Chem (1996) 39: 1560-1563 [PMID:8691489] |
ChEMBL | Inhibition of [3H]dopamine uptake at human DAT M272L/R344M mutant expressed in HEK293 cells | B | 5.93 | pIC50 | 1172 | nM | IC50 | J Biol Chem (2007) 282: 8915-8925 [PMID:17255098] |
ChEMBL | Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells | B | 5.97 | pIC50 | 1060 | nM | IC50 | J Biol Chem (2007) 282: 8915-8925 [PMID:17255098] |
ChEMBL | Inhibition of [3H]dopamine uptake at human DAT M272L/1291M/R344M mutant expressed in HEK293 cells | B | 6.12 | pIC50 | 759 | nM | IC50 | J Biol Chem (2007) 282: 8915-8925 [PMID:17255098] |
ChEMBL | Displacement of [3H]WIN35428 from human DAT transfected cell membrane | B | 6.17 | pIC50 | 670 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 48-51 [PMID:21146984] |
ChEMBL | Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay | B | 6.19 | pIC50 | 645.65 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445] |
ChEMBL | Inhibition of [3H]dopamine reuptake at human DAT expressed in HEK cells | B | 6.23 | pIC50 | 590 | nM | IC50 | Bioorg Med Chem (2009) 17: 2047-2068 [PMID:19201198] |
ChEMBL | Inhibition of [3H]dopamine uptake at human DAT R344M mutant expressed in HEK293 cells | B | 6.29 | pIC50 | 507 | nM | IC50 | J Biol Chem (2007) 282: 8915-8925 [PMID:17255098] |
ChEMBL | Inhibition of [3H]DA uptake in DAT | B | 6.32 | pIC50 | 478 | nM | IC50 | J Med Chem (2008) 51: 2795-2806 [PMID:18393401] |
ChEMBL | Inhibition of [3H] dopamine uptake into human DAT expressed in HEK293 cells | F | 6.34 | pIC50 | 461 | nM | IC50 | J Med Chem (2006) 49: 1420-1432 [PMID:16480278] |
ChEMBL | Inhibitory activity against [3H]-Dopamine uptake from Dopamine transporter in rat caudate putamen tissue | B | 6.39 | pIC50 | 405 | nM | IC50 | J Med Chem (1996) 39: 1560-1563 [PMID:8691489] |
ChEMBL | Displacement of [3H]CFT from human DAT expressed in HEK293 cells | B | 6.41 | pIC50 | 392 | nM | IC50 | J Biol Chem (2007) 282: 8915-8925 [PMID:17255098] |
ChEMBL | Displacement of [125I]-RTI-55 from Dopamine transporter expressed in HEK293 cells | B | 6.44 | pIC50 | 367 | nM | IC50 | J Med Chem (2005) 48: 2876-2881 [PMID:15828826] |
ChEMBL | Displacement of [3H]CFT from human DAT M272L/R344M mutant expressed in HEK293 cells | B | 6.44 | pIC50 | 366 | nM | IC50 | J Biol Chem (2007) 282: 8915-8925 [PMID:17255098] |
ChEMBL | Inhibition of [3H]dopamine uptake in HEK cells expressing human DAT | B | 6.48 | pIC50 | 330 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4133-4137 [PMID:14592523] |
ChEMBL | Inhibition of [3H]DA from human recombinant DAT expressed in HEK293 cells | B | 6.52 | pIC50 | 303 | nM | IC50 | Bioorg Med Chem (2009) 17: 337-343 [PMID:19014888] |
ChEMBL | Displacement of [3H]dopamine from human recombinant DAT expressed in HEK293 cells by scintillation counting | B | 6.52 | pIC50 | 303 | nM | IC50 | J Med Chem (2009) 52: 1530-1539 [PMID:19256502] |
ChEMBL | Inhibition of [3H]dopamine uptake in HEK cells expressing human Dopamine transporter | B | 6.52 | pIC50 | 301 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 297-300 [PMID:10698458] |
ChEMBL | Inhibition of dopamine uptake in HEK cells expressing human dopamine transporter (hDAT) | F | 6.53 | pIC50 | 296 | nM | IC50 | J Med Chem (2002) 45: 4097-4109 [PMID:12213053] |
ChEMBL | Inhibition of [3H]dopamine uptake in HEK293 cells expressing human dopamine transporter | F | 6.54 | pIC50 | 289 | nM | IC50 | J Med Chem (2005) 48: 2876-2881 [PMID:15828826] |
ChEMBL | Displacement of [3H]CFT from human DAT R344M mutant expressed in HEK293 cells | B | 6.55 | pIC50 | 283 | nM | IC50 | J Biol Chem (2007) 282: 8915-8925 [PMID:17255098] |
ChEMBL | Inhibition of recombinant human DAT expressed in HEK293 cell membranes assessed as reduction in [3H]-DA uptake incubated for 22 mins by micro beta scintillation counting analysis | B | 6.56 | pIC50 | 274 | nM | IC50 | J Med Chem (2017) 60: 3109-3123 [PMID:28319392] |
ChEMBL | Inhibition of [3H]dopamine reuptake at human DAT expressed in HEK293 cells | B | 6.57 | pIC50 | 267 | nM | IC50 | J Med Chem (2009) 52: 6768-6781 [PMID:19821577] |
ChEMBL | Compound was tested for inhibition of [3H]DA binding to Dopamine transporter in HEK cells | B | 6.57 | pIC50 | 267 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2151-2154 [PMID:12798324] |
ChEMBL | Displacement of [3H]CFT from human DAT M272L/1291M/R344M mutant expressed in HEK293 cells | B | 6.59 | pIC50 | 259 | nM | IC50 | J Biol Chem (2007) 282: 8915-8925 [PMID:17255098] |
ChEMBL | Inhibition of [3H]DA uptake at human DAT expressing HEK293 cells | B | 6.62 | pIC50 | 240 | nM | IC50 | J Med Chem (2007) 50: 219-232 [PMID:17228864] |
ChEMBL | Inhibition of [3H]DA reuptake at human DAT expressed in HEK293 cells | B | 6.64 | pIC50 | 227 | nM | IC50 | Bioorg Med Chem (2009) 17: 6890-6897 [PMID:19740668] |
ChEMBL | Inhibition of [3H]dopamine reuptake in HEK293 cells expressing human dopamine transporter | B | 6.72 | pIC50 | 190 | nM | IC50 | J Med Chem (2000) 43: 205-213 [PMID:10649976] |
ChEMBL | Inhibition of [3H]DA uptake in HEK cells expressing dopamine transporter | F | 6.72 | pIC50 | 190 | nM | IC50 | J Med Chem (1999) 42: 3647-3656 [PMID:10479296] |
ChEMBL | Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells | B | 6.89 | pIC50 | 130 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 4133-4140 [PMID:17846138] |
ChEMBL | Inhibition of [3H]3-beta-(4-fluorophenyl)tropane-2beta-carboxylic acid methyl ester binding to dopamine transporter of cynomolgus monkey striatum | B | 7.02 | pIC50 | 95.6 | nM | IC50 | J Med Chem (1993) 36: 855-862 [PMID:8464040] |
ChEMBL | Displacement of [3H]WIN-35428 from human DAT | B | 7.05 | pIC50 | 89.1 | nM | IC50 | J Med Chem (2006) 49: 4589-4594 [PMID:16854064] |
ChEMBL | Displacement of [3H]WIN-35428 from dopamine transporter | B | 7.05 | pIC50 | 89.1 | nM | IC50 | Bioorg Med Chem (2008) 16: 5529-5535 [PMID:18434164] |
ChEMBL | Displacement of [3H]WIN-35428 from DAT | B | 7.05 | pIC50 | 89.1 | nM | IC50 | J Med Chem (2005) 48: 7437-7444 [PMID:16279803] |
ChEMBL | Displacement of [3H]WIN-35428 from DAT | B | 7.05 | pIC50 | 89.1 | nM | IC50 | J Med Chem (2004) 47: 6401-6409 [PMID:15566309] |
ChEMBL | Displacement of [3H]WIN-35428 from DAT | B | 7.05 | pIC50 | 89.1 | nM | IC50 | Bioorg Med Chem (2009) 17: 5126-5132 [PMID:19523837] |
Dopamine transporter in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2986] [UniProtKB: P27922] | ||||||||
ChEMBL | Competitive inhibition against [3H]cocaine binding to cocaine receptor in bovine striatal tissue | B | 6.86 | pIC50 | 139 | nM | IC50 | J Med Chem (1990) 33: 2024-2028 [PMID:2362282] |
ChEMBL | In vitro inhibitory activity towards [3H]cocaine binding to rat striatal tissue | B | 7.19 | pIC50 | 65 | nM | IC50 | J Med Chem (1991) 34: 702-705 [PMID:1995895] |
DAT/Dopamine transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2799] [GtoPdb: 927] [UniProtKB: Q61327] | ||||||||
ChEMBL | Inhibition of [125I]RTI-55 binding to mouse DAT expressed in HEK293 cells preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis | B | 6.07 | pKi | 850 | nM | Ki | J Med Chem (2017) 60: 3109-3123 [PMID:28319392] |
ChEMBL | Inhibition of mouse DAT expressed in HEK293 cells assessed as reduction in [3H]-DA uptake | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2017) 60: 3109-3123 [PMID:28319392] |
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
ChEMBL | Inhibition of [3H]WIN-35428 binding to rat dopamine transporter | B | 4.49 | pKi | 32000 | nM | Ki | J Med Chem (2005) 48: 1336-1343 [PMID:15743177] |
ChEMBL | Inhibitory constant towards reuptake of [125I]-13 from dopamine transporter in rat striatal membranes | B | 6.19 | pKi | 642 | nM | Ki | J Med Chem (1994) 37: 1535-1542 [PMID:8182712] |
ChEMBL | Binding affinity for dopamine transporters in rat brain tissue. | B | 6.29 | pKi | 510 | nM | Ki | J Med Chem (1994) 37: 1558-1561 [PMID:8201589] |
ChEMBL | Displacement of [125I]RTI-55 from Dopamine transporter of rat caudate membranes | B | 6.34 | pKi | 460 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2225-2228 [PMID:12127543] |
ChEMBL | Ability to inhibit reuptake of dopamine ([3H]DA) at dopamine transporter of rat striatum | B | 6.37 | pKi | 423 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 3565-3569 [PMID:14505672] |
ChEMBL | Ability to inhibit [3H]DA reuptake at dopamine transporter from rat brain | B | 6.37 | pKi | 423 | nM | Ki | J Med Chem (2003) 46: 1997-2007 [PMID:12723962] |
ChEMBL | Inhibition of high affinity uptake by the dopamine transporter from rat synaptosomal nerve endings by using [3H]DA as radioligand | B | 6.37 | pKi | 423 | nM | Ki | J Med Chem (2004) 47: 5821-5824 [PMID:15537337] |
ChEMBL | Inhibition of [3H]DA uptake by dopamine transporter of rat striata synaptosomes | B | 6.37 | pKi | 423 | nM | Ki | J Med Chem (2000) 43: 1215-1222 [PMID:10737754] |
ChEMBL | Inhibition of high affinity DA uptake into rat synaptosomes using [3H]DA | B | 6.37 | pKi | 423 | nM | Ki | J Med Chem (2001) 44: 1615-1622 [PMID:11334571] |
ChEMBL | Ability to inhibit high affinity reuptake of [3H]DA from dopamine transporter into nerve endings synaptosomes | B | 6.37 | pKi | 423 | nM | Ki | J Med Chem (2002) 45: 1930-1941 [PMID:11960503] |
ChEMBL | Binding affinity for [3H]DA (Dopamine transporter) uptake by striated synaptosomes | B | 6.37 | pKi | 423 | nM | Ki | J Med Chem (1998) 41: 4973-4982 [PMID:9836615] |
ChEMBL | Inhibition of high affinity uptake of [3H]dopamine into nerve endings (synaptosomes) prepared from various regions of the rat brain. | B | 6.37 | pKi | 423 | nM | Ki | J Med Chem (2000) 43: 3283-3294 [PMID:10966747] |
ChEMBL | Inhibition of reuptake of [3H]DA at Dopamine transporter (DAT) | B | 6.37 | pKi | 423 | nM | Ki | J Med Chem (2000) 43: 2064-2071 [PMID:10821718] |
ChEMBL | Compound was tested for its ability to inhibit high affinity uptake of [3H]DA into rat striatal membrane | B | 6.38 | pKi | 420 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1443-1446 [PMID:10888328] |
ChEMBL | Inhibition of [3H]dopamine uptake at striatal nerve endings by dopamine transporter | B | 6.38 | pKi | 420 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 3325-3328 [PMID:10612593] |
ChEMBL | Binding affinity towards dopamine transporter using [3H]WIN-35428 as radioligand in rat caudate-putamen tissue | B | 6.41 | pKi | 390 | nM | Ki | J Med Chem (1998) 41: 2430-2435 [PMID:9632375] |
ChEMBL | Binding affinity against dopamine transporter in rat caudate putamen tissue using [3H]WIN-35428 radioligand. | B | 6.41 | pKi | 390 | nM | Ki | J Med Chem (1996) 39: 4744-4749 [PMID:8941387] |
ChEMBL | Binding affinity was determined against cocaine receptor by measuring the ability of compound to displace bound [3H]-3 from rat caudate-putamen tissue | B | 6.41 | pKi | 388 | nM | Ki | J Med Chem (1994) 37: 3875-3877 [PMID:7966147] |
ChEMBL | Displacement of [3H]WIN-35428 binding to the dopamine transporter (DAT) in Rat Caudate Putamen | B | 6.41 | pKi | 388 | nM | Ki | J Med Chem (1997) 40: 851-857 [PMID:9083473] |
ChEMBL | Displacement of [3H]WIN-35428 from dopamine transporter (DAT) in Rat Caudate Putamen | B | 6.41 | pKi | 388 | nM | Ki | J Med Chem (1997) 40: 858-863 [PMID:9083474] |
ChEMBL | Compound was evaluated for its ability to displace [3H]WIN-35428 binding in rat caudate-putamen | B | 6.41 | pKi | 388 | nM | Ki | J Med Chem (1994) 37: 2258-2261 [PMID:8057273] |
ChEMBL | In vitro binding affinity towards dopamine transporter in rat striatal membranes by [3H]GBR-12395 displacement. | B | 6.46 | pKi | 350 | nM | Ki | J Med Chem (1996) 39: 543-548 [PMID:8558525] |
ChEMBL | Inhibition of high affinity uptake of [3H]dopamine into striatal nerve endings (synaptosomes) | B | 6.49 | pKi | 320 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1831-1836 [PMID:10406650] |
ChEMBL | Inhibition of [3H]DA binding to dopamine transporter of rat brain synaptosomes | B | 6.52 | pKi | 301 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1681-1686 [PMID:10937724] |
ChEMBL | Binding affinity at dopamine transporter in rat brain by [3H]WIN-35428 displacement. | B | 6.55 | pKi | 285 | nM | Ki | J Med Chem (2004) 47: 3388-3398 [PMID:15189035] |
ChEMBL | In vitro dopamine transporter binding affinity using [3H]WIN-35428 as radioligand was determined | B | 6.55 | pKi | 285 | nM | Ki | J Med Chem (2003) 46: 2908-2916 [PMID:12825932] |
ChEMBL | Binding affinity of compound on dopamine transporters of rat striated membranes using [3H]- mazindol. | B | 6.55 | pKi | 281 | nM | Ki | J Med Chem (1998) 41: 4973-4982 [PMID:9836615] |
ChEMBL | Binding affinity to inhibit [3H]mazindol binding in rat corpus striatum P2 synaptosomes | B | 6.55 | pKi | 280 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 303-308 |
ChEMBL | Binding affinity was tested by measuring its ability to displace [3H]mazindol binding against dopamine transporter (DAT) of rat striatal membranes | B | 6.55 | pKi | 280 | nM | Ki | J Med Chem (1994) 37: 3440-3442 [PMID:7932572] |
ChEMBL | ability to displace [3H]- Mazindol binding to cocaine binding sites on Dopamine transporter of rat striatal membranes | B | 6.55 | pKi | 280 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1443-1446 [PMID:10888328] |
ChEMBL | Binding affinity towards dopamine transporter using [3H]- mazindol as radioligand in rat striatal membranes | B | 6.55 | pKi | 280 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1831-1836 [PMID:10406650] |
ChEMBL | Inhibition of [3H]DA Uptake was measured by liquid scintillation spectrometry | B | 6.56 | pKi | 274 | nM | Ki | J Med Chem (2000) 43: 351-360 [PMID:10669562] |
ChEMBL | Inhibition of [3H]DA uptake at Dopamine transporter in rat cortex. | B | 6.57 | pKi | 270 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1113-1118 [PMID:11354356] |
ChEMBL | Inhibition of [3H]DA reuptake at dopamine transporter in rat striatum | B | 6.59 | pKi | 259 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 993-995 [PMID:11909701] |
ChEMBL | Inhibition of high affinity uptake of [3H]DA using rat nerve endings obtained from brain regions enriched in DAT. | B | 6.59 | pKi | 259 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2079-2083 [PMID:11514143] |
ChEMBL | Inhibition of high affinity uptake of [3H]-DA by dopamine transporter in nerve endings obtained from rat brain. | B | 6.59 | pKi | 259 | nM | Ki | J Med Chem (2002) 45: 3161-3170 [PMID:12109901] |
ChEMBL | Ability to inhibit high affinity uptake of [3H]DA at Dopamine transporter (DAT) using rat brain striatum | B | 6.59 | pKi | 259 | nM | Ki | J Med Chem (2004) 47: 3009-3018 [PMID:15163183] |
ChEMBL | Inhibition of [3H]DA uptake by rat striatal dopamine transporter | B | 6.62 | pKi | 241.3 | nM | Ki | J Med Chem (1995) 38: 379-388 [PMID:7830281] |
ChEMBL | Displacement of [3H]WIN-35428 from DAT in rat brain | B | 6.63 | pKi | 237 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6865-6868 [PMID:19896846] |
ChEMBL | Displacement of [3H]mazindol from cocaine binding site on Dopamine transporter (DAT) | B | 6.64 | pKi | 230 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 3325-3328 [PMID:10612593] |
ChEMBL | Displacement of [3H]mazindol binding to dopamine transporter (DAT) in rat synaptosomes | B | 6.64 | pKi | 230 | nM | Ki | J Med Chem (2001) 44: 1615-1622 [PMID:11334571] |
ChEMBL | Inhibition of [3H]mazindol binding to dopamine transporter of rat striatal membranes. | B | 6.64 | pKi | 230 | nM | Ki | J Med Chem (2000) 43: 3283-3294 [PMID:10966747] |
ChEMBL | Inhibition of [3H]- Mazindol binding to dopamine transporter of rat striatal membrane. | B | 6.64 | pKi | 230 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1681-1686 [PMID:10937724] |
ChEMBL | Displacement of [3H]WIN-35428 from dopamine transporter of rat caudate putamen tissue | B | 6.73 | pKi | 187 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2387-2390 [PMID:12161139] |
ChEMBL | Binding affinity Sprague-Dawley rats using [3H]WIN-35428 ligand | B | 6.73 | pKi | 187 | 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 | 6.73 | pKi | 187 | nM | Ki | J Med Chem (2003) 46: 2589-2598 [PMID:12801223] |
ChEMBL | Displacement of [3H]WIN-35248 from dopamine transporter (DAT) of rat striatal membrane | B | 6.84 | pKi | 146 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2079-2083 [PMID:11514143] |
ChEMBL | Inhibition of [3H]dopamine uptake at DAT in Sprague-Dawley rat striatum synaptosome | B | 6.95 | pKi | 111 | nM | Ki | Bioorg Med Chem (2007) 15: 3748-3755 [PMID:17399987] |
ChEMBL | Displacement of [3H]GBR-12935 from dopamine transporter of rat caudate-putamen | B | 7.05 | pKi | 89 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1131-1133 [PMID:15686927] |
ChEMBL | Displacement of [3H]WIN-from DAT in rat brain membrane | B | 7.13 | pKi | 74.3 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 5419-5423 [PMID:16213721] |
ChEMBL | Displacement of [3H]WIN-35428 from dopamine transporter of rat brain membrane | B | 7.13 | pKi | 74.3 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 3295-3298 [PMID:15149693] |
ChEMBL | Displacement of [3H]WIN35428 from DAT in Sprague-Dawley rat brain membranes | B | 7.14 | pKi | 71.8 | nM | Ki | ACS Med Chem Lett (2011) 2: 48-52 [PMID:21344069] |
ChEMBL | Displacement of [3H]WIN-35428 from DAT in Sprague-Dawley rat brain | B | 7.14 | pKi | 71.8 | nM | Ki | J Med Chem (2006) 49: 6391-6399 [PMID:17034144] |
ChEMBL | Binding affinity towards dopamine transporter using [3H]WIN-35428 as radioligand in rat caudate-putamen tissue | B | 7.49 | pKi | 32 | nM | Ki | J Med Chem (1998) 41: 2430-2435 [PMID:9632375] |
ChEMBL | Binding affinity against dopamine transporter in rat caudate putamen tissue using [3H]WIN-35428 radioligand. (from other reference) | B | 7.49 | pKi | 32 | nM | Ki | J Med Chem (1996) 39: 4744-4749 [PMID:8941387] |
ChEMBL | Affinity for rat dopamine transporter using [3H]WIN-35428 displacement. | B | 7.49 | pKi | 32 | nM | Ki | J Med Chem (1995) 38: 3933-3940 [PMID:7562926] |
ChEMBL | Binding affinity was determined against cocaine receptor by measuring the ability of compound to displace bound [3H]-3 from rat caudate-putamen tissue | B | 7.49 | pKi | 32 | nM | Ki | J Med Chem (1994) 37: 3875-3877 [PMID:7966147] |
ChEMBL | Affinity for dopamine transporter was assessed by the ability to displace [3H]WIN-35428 from rat caudate-putamen tissue | B | 7.49 | pKi | 32 | nM | Ki | J Med Chem (2002) 45: 1203-1210 [PMID:11881989] |
ChEMBL | Displacement of [3H]WIN-35428 from dopamine transporter (DAT) in Rat Caudate Putamen | B | 7.49 | pKi | 32 | nM | Ki | J Med Chem (1997) 40: 858-863 [PMID:9083474] |
ChEMBL | Displacement of [3H]WIN-35428 from dopamine transporter in rat caudate putamen tissue | B | 7.49 | pKi | 32 | nM | Ki | J Med Chem (1997) 40: 4406-4414 [PMID:9435910] |
ChEMBL | Inhibition of [3H]WIN-35428 binding to dopamine transporter in rat striatal membranes. | B | 4.8 | pIC50 | 15800 | nM | IC50 | J Med Chem (1993) 36: 3572-3579 [PMID:8246225] |
ChEMBL | Inhibition of [3H]WIN-35428 binding to rat striatal membrane dopamine transporter | B | 4.8 | pIC50 | 15800 | nM | IC50 | J Med Chem (1991) 34: 883-886 [PMID:2002468] |
ChEMBL | Inhibition of [3H]WIN-35065-2 binding to the dopamine transporter. | B | 5.74 | pIC50 | 1810 | nM | IC50 | J Med Chem (1992) 35: 969-981 [PMID:1552510] |
ChEMBL | Inhibition of [3H]GBR-12935 binding to the dopamine transporter. | B | 5.84 | pIC50 | 1450 | nM | IC50 | J Med Chem (1992) 35: 969-981 [PMID:1552510] |
ChEMBL | Inhibition of [3H]dopamine uptake at the dopamine transporter. | B | 6.07 | pIC50 | 843 | nM | IC50 | J Med Chem (1992) 35: 969-981 [PMID:1552510] |
ChEMBL | Binding against Dopamine transporter using radioligand as [3H]GBR 12935 | B | 6.18 | pIC50 | 660 | nM | IC50 | J Med Chem (1996) 39: 4704-4716 [PMID:8941383] |
ChEMBL | Compound was evaluated for its ability to displace [3H]mazindol binding from rat striatal membranes | B | 6.24 | pIC50 | 580 | nM | IC50 | J Med Chem (1992) 35: 4764-4766 [PMID:1469704] |
ChEMBL | Inhibition of [3H]WIN-35428 binding to Dopamine transporter in rat striatal synaptic membranes | B | 6.29 | pIC50 | 510.6 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 3077-3080 [PMID:11714614] |
ChEMBL | Inhibition of dopamine DA reuptake | B | 6.32 | pIC50 | 478 | nM | IC50 | J Med Chem (1996) 39: 4704-4716 [PMID:8941383] |
ChEMBL | Inhibitory activity determined for [3H]DA (Dopamine transporter) uptake by striated synaptosomes | B | 6.34 | pIC50 | 459 | nM | IC50 | J Med Chem (1998) 41: 4973-4982 [PMID:9836615] |
ChEMBL | Tested for its ability to inhibit high affinity uptake of [3H]dopamine into rat caudate-putamen tissue | B | 6.39 | pIC50 | 405 | nM | IC50 | J Med Chem (1994) 37: 3875-3877 [PMID:7966147] |
ChEMBL | Inhibition of dopamine uptake into rat striatal tissue, using [3H]- dopamine as the radioligand. | B | 6.39 | pIC50 | 404 | nM | IC50 | J Med Chem (1999) 42: 882-895 [PMID:10072685] |
ChEMBL | Inhibition of [3H]DA binding to DAT in rat striatal synaptosomes. | B | 6.39 | pIC50 | 404 | nM | IC50 | J Med Chem (2003) 46: 1456-1464 [PMID:12672245] |
ChEMBL | Inhibitory potency against [3H]DA uptake using [3H]WIN-35428 (WIN-) binding assay | B | 6.39 | pIC50 | 404 | nM | IC50 | J Med Chem (1999) 42: 4836-4843 [PMID:10579846] |
ChEMBL | Inhibitory activity against [3H]dopamine uptake in rat striatal tissue | F | 6.39 | pIC50 | 404 | nM | IC50 | J Med Chem (1996) 39: 1201-1209 [PMID:8632426] |
ChEMBL | Inhibitory activity on dopamine transporters of rat striated membranes using [3H]- mazindol. | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (1998) 41: 4973-4982 [PMID:9836615] |
ChEMBL | Inhibition of [3H]dopamine uptake into rat striatal synaptosomes | F | 6.45 | pIC50 | 353.1 | nM | IC50 | J Med Chem (2005) 48: 3337-3343 [PMID:15857139] |
ChEMBL | Compound was tested for binding against Dopamine transporter using radioligand as [3H]-RTI 55 | B | 6.47 | pIC50 | 341 | nM | IC50 | J Med Chem (1996) 39: 4704-4716 [PMID:8941383] |
ChEMBL | Affinity for dopamine transporter was assessed by the ability to displace [3H]WIN-35428 from rat caudate-putamen tissue | B | 6.47 | pIC50 | 338 | nM | IC50 | J Med Chem (2002) 45: 1203-1210 [PMID:11881989] |
ChEMBL | Compound was evaluated for its ability to displace [3H]WIN-35428 from dopamine transporter in rat caudate putamen tissue | B | 6.47 | pIC50 | 338 | nM | IC50 | J Med Chem (1997) 40: 4406-4414 [PMID:9435910] |
ChEMBL | Inhibition of rat DAT-mediated [3H]dopamine uptake in CHO cells | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2006) 49: 4048-4051 [PMID:16821765] |
ChEMBL | Functional cocaine antagonism was evaluated by inhibition of [3H]dopamine reuptake | F | 6.53 | pIC50 | 297 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 1113-1118 [PMID:11354356] |
ChEMBL | Tested for inhibition of radioligand [3H]dopamine (DA) uptake in rat synaptosomes | B | 6.53 | pIC50 | 296 | nM | IC50 | J Med Chem (1993) 36: 4075-4081 [PMID:8258830] |
ChEMBL | Inhibition of [3H]WIN-35428 binding to dopamine transporter of rat striatum | B | 6.58 | pIC50 | 266 | nM | IC50 | J Med Chem (2004) 47: 5101-5113 [PMID:15456254] |
ChEMBL | Binding affinity was evaluated by measuring the inhibition of [3H]WIN-35428 binding to Dopamine transporter in rat brain tissue | B | 6.58 | pIC50 | 266 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2337-2340 [PMID:11527726] |
ChEMBL | In vitro binding affinity at dopamine transporter in rat striatum by [3H]WIN-35428 displacement. | B | 6.58 | pIC50 | 266 | nM | IC50 | J Med Chem (2001) 44: 937-948 [PMID:11300876] |
ChEMBL | Binding affinity at the dopamine transporter in rast striatum by [3H]WIN-35428 displacement. | B | 6.58 | pIC50 | 266 | nM | IC50 | J Med Chem (2003) 46: 2205-2215 [PMID:12747792] |
ChEMBL | Inhibition of binding of [3H]WIN-35 428 to (DAT) dopamine transporter in rat striatum | B | 6.58 | pIC50 | 266 | 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 | 6.58 | pIC50 | 266 | nM | IC50 | J Med Chem (2003) 46: 1220-1228 [PMID:12646032] |
ChEMBL | Inhibition of binding of 3[H] WIN-35 428 to Dopamine transporter (DAT) of rat striatum. | B | 6.58 | pIC50 | 266 | nM | IC50 | J Med Chem (2002) 45: 654-662 [PMID:11806716] |
ChEMBL | Inhibition of dopamine Transporter Affinity against rat whole brain using [3H]WIN-35428 as radioligand | B | 6.6 | pIC50 | 249 | nM | IC50 | J Med Chem (1998) 41: 2380-2389 [PMID:9632371] |
ChEMBL | Compound was tested for inhibitory activity to displace [3H]WIN-35428 at dopamine transporter in Rat Striatal Membranes. | B | 6.6 | pIC50 | 249 | nM | IC50 | J Med Chem (1997) 40: 2474-2481 [PMID:9258354] |
ChEMBL | Inhibition of high-affinity uptake of [3H]dopamine at dopamine transporter into rat striatal nerve endings (synaptosomes) | B | 6.62 | pIC50 | 239 | nM | IC50 | J Med Chem (1998) 41: 1962-1969 [PMID:9599245] |
ChEMBL | In vitro potency for inhibiting [3H]- dopamine uptake was determined | F | 6.63 | pIC50 | 236 | nM | IC50 | J Med Chem (2003) 46: 2908-2916 [PMID:12825932] |
ChEMBL | Inhibition of [3H]dopamine uptake at DAT in Sprague-Dawley rat brain | B | 6.63 | pIC50 | 236 | nM | IC50 | J Med Chem (2006) 49: 6391-6399 [PMID:17034144] |
ChEMBL | Inhibition of [3H]WIN-35428 binding to rat DAT expressed in D8 cells | B | 6.65 | pIC50 | 226 | nM | IC50 | J Med Chem (2006) 49: 4048-4051 [PMID:16821765] |
ChEMBL | Compound was tested for binding affinity to dopamine reuptake sites in the tissue homogenates prepared from primate rat striatum using [3H]CFT as radioligand | B | 6.66 | pIC50 | 221 | nM | IC50 | J Med Chem (1991) 34: 3144-3146 [PMID:1920365] |
ChEMBL | Inhibition [3H]DA uptake in rat striatal synaptosomes. | F | 6.68 | pIC50 | 209 | nM | IC50 | J Med Chem (1998) 41: 864-876 [PMID:9526561] |
ChEMBL | Inhibition of Dopamine uptake in male Sprague-Dawley rats using [3H]DA ligand | B | 6.69 | pIC50 | 205 | nM | IC50 | J Med Chem (1999) 42: 4446-4455 [PMID:10543888] |
ChEMBL | Binding affinity for compound at site labeled by [3H]BTCP (1-[1-(2-benxo[b]thienyl)cyclohexyl]piperidine) in rat forebrain. | B | 6.73 | pIC50 | 187 | nM | IC50 | J Med Chem (1993) 36: 1188-1193 [PMID:8098066] |
ChEMBL | Tested for radioligand [3H]BTCP displacement from dopamine transporter in rat forebrain | B | 6.75 | pIC50 | 179 | nM | IC50 | J Med Chem (1993) 36: 4075-4081 [PMID:8258830] |
ChEMBL | Inhibition of [3H]WIN-35428 binding to dopamine transporter in rat striatal tissue | B | 6.76 | pIC50 | 173 | nM | IC50 | J Med Chem (1996) 39: 1201-1209 [PMID:8632426] |
ChEMBL | Inhibitory binding activity against rat striatal tissue using [3H]WIN-35248 as the radioligand. | B | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (1999) 42: 882-895 [PMID:10072685] |
ChEMBL | Inhibitory potency against dopamine (DA) transporter using [3H]WIN-35428 (WIN-) binding assay. | B | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (1999) 42: 4836-4843 [PMID:10579846] |
ChEMBL | Inhibition of [3H]WIN-35428 binding to the cocaine binding site on the dopamine transporter (DAT) in synaptosomal membrane preparations from rat striatal tissue. | B | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (2003) 46: 1456-1464 [PMID:12672245] |
ChEMBL | Inhibition of [3H]WIN-35428 binding to the dopamine transporter. | B | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (1992) 35: 969-981 [PMID:1552510] |
ChEMBL | Displacement of [3H]WIN-35428 from Dopamine transporter of rat caudate putamen | B | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2005) 48: 3337-3343 [PMID:15857139] |
ChEMBL | Inhibition of [3H]cocaine binding to the dopamine transporter. | B | 6.86 | pIC50 | 139 | nM | IC50 | J Med Chem (1992) 35: 969-981 [PMID:1552510] |
ChEMBL | Binding affinity of compound at site labeled by [3H]-cocaine in rat forebrain. | B | 6.97 | pIC50 | 107 | nM | IC50 | J Med Chem (1993) 36: 1188-1193 [PMID:8098066] |
ChEMBL | Displacement of [125I]RTI-55 dopamine transporter binding in rat striatal membrane | B | 6.98 | pIC50 | 104 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4915-4918 [PMID:16165350] |
ChEMBL | Inhibition of [3H]WIN-35428 binding to dopamine transporter in rat striatal membranes. | B | 6.99 | pIC50 | 102 | nM | IC50 | J Med Chem (1993) 36: 3572-3579 [PMID:8246225] |
ChEMBL | Ability to displace [3H]WIN-35428 binding to dopamine transporter from rat striatal membranes | B | 6.99 | pIC50 | 102 | nM | IC50 | J Med Chem (1998) 41: 1962-1969 [PMID:9599245] |
ChEMBL | Inhibition of [3H]3-beta-(p-fluorophenyl)tropane-2beta-carboxylic acid methyl ester binding to Dopamine transporter in rat striatal membranes. | B | 6.99 | pIC50 | 102 | nM | IC50 | J Med Chem (1992) 35: 135-140 [PMID:1732520] |
ChEMBL | Inhibition of [3H]3-beta-(p-fluorophenyl)tropane-2beta-carboxylic acid methyl ester [3H]7a binding to Dopamine transporter of rat striatal membranes | B | 6.99 | pIC50 | 102 | nM | IC50 | J Med Chem (1992) 35: 141-144 [PMID:1732521] |
ChEMBL | Inhibition of [3H]WIN-35248 binding to the dopamine transporter in rat striatal membranes. | B | 6.99 | pIC50 | 102 | nM | IC50 | J Med Chem (1992) 35: 1813-1817 [PMID:1588560] |
ChEMBL | Inhibition of [3H]WIN-35428l binding to Dopamine transporter | B | 6.99 | pIC50 | 102 | nM | IC50 | J Med Chem (1992) 35: 2497-2500 [PMID:1619622] |
ChEMBL | Inhibition of [3H]WIN-35428 binding to rat striatal membrane dopamine transporter | B | 6.99 | pIC50 | 102 | nM | IC50 | J Med Chem (1991) 34: 883-886 [PMID:2002468] |
ChEMBL | Inhibition of [3H]cocaine binding to Cocaine receptor in rat striatal membranes | B | 7 | pIC50 | 101 | nM | IC50 | J Med Chem (1998) 41: 864-876 [PMID:9526561] |
ChEMBL | Displacement of 0.5 nM [3H]WIN-35248 from Dopamine transporter | B | 7.05 | pIC50 | 89.1 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2445-2447 [PMID:11078197] |
ChEMBL | Inhibition of [3H]WIN-35428 binding to Dopamine transporter | B | 7.05 | pIC50 | 89.1 | nM | IC50 | J Med Chem (1996) 39: 4139-4141 [PMID:8863789] |
ChEMBL | In vitro inhibitory activity against radioligand [3H]-WN 35,428 binding to dopamine transporter (DAT) in rat striatal tissue | B | 7.05 | pIC50 | 89.1 | nM | IC50 | J Med Chem (1997) 40: 3861-3864 [PMID:9397165] |
ChEMBL | Inhibitory concentration required to inhibit dopamine transporter DAT was determined by using [3H]WIN-35428 radioligand | B | 7.05 | pIC50 | 89.1 | nM | IC50 | J Med Chem (2004) 47: 296-302 [PMID:14711303] |
ChEMBL | Ability to displace [3H]WIN-35428 from Dopamine Transporter of rat striatal membrane | B | 7.05 | pIC50 | 89.1 | nM | IC50 | J Med Chem (2002) 45: 4097-4109 [PMID:12213053] |
ChEMBL | Inhibition of [3H]WIN-35428 binding to dopamine (DA) transporter | B | 7.05 | pIC50 | 89.1 | nM | IC50 | J Med Chem (1994) 37: 1220-1223 [PMID:8164265] |
ChEMBL | Inhibition of [3H]WIN-35428 binding to rat striatal dopamine transporter | B | 7.05 | pIC50 | 89.1 | nM | IC50 | J Med Chem (2005) 48: 3852-3857 [PMID:15916437] |
ChEMBL | Inhibition of [3H]WIN-35428 binding to the dopamine transporter in rat striata. | B | 7.05 | pIC50 | 89 | nM | IC50 | J Med Chem (1996) 39: 4027-4035 [PMID:8831768] |
ChEMBL | Inhibition of [3H]WIN-35428 binding at dopamine transporter was determined | B | 7.05 | pIC50 | 89 | nM | IC50 | J Med Chem (2003) 46: 1775-1794 [PMID:12723940] |
ChEMBL | Compound was tested for its ability to inhibit the neurotransmitter dopamine-DA reuptake system using [3H]dopamine as radioligand | B | 7.05 | pIC50 | 89 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 2559-2564 |
ChEMBL | Ability to inhibit binding of [3H]WIN-35428 to dopamine transporter in rat caudate putamen | B | 7.05 | pIC50 | 89 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 823-827 [PMID:11277529] |
ChEMBL | Binding affinity at the Dopamine transporter in rat striata by inhibition of 0.5 nM [3H]WIN-35428 binding | B | 7.05 | pIC50 | 89 | nM | IC50 | J Med Chem (1995) 38: 379-388 [PMID:7830281] |
ChEMBL | Inhibitory activity against Dopamine transporter using 0.5 nM [3H]WIN-35428 as radioligand | B | 7.05 | pIC50 | 89 | nM | IC50 | J Med Chem (1997) 40: 1247-1251 [PMID:9111298] |
ChEMBL | Inhibitory activity against radioligand [3H]WIN-35428 binding at the dopamine transporter | B | 7.05 | pIC50 | 89 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 3689-3692 [PMID:9934496] |
ChEMBL | Binding affinity towards dopamine transporter was determined using DA[3H]WIN-35428 as radioligand | B | 7.05 | pIC50 | 89 | nM | IC50 | J Med Chem (1995) 38: 3451-3453 [PMID:7658431] |
ChEMBL | Tested for radioligand [3H]cocaine displacement from dopamine transporter in rat forebrain | B | 7.09 | pIC50 | 82 | nM | IC50 | J Med Chem (1993) 36: 4075-4081 [PMID:8258830] |
GtoPdb | - | - | 7.1 | pIC50 | 89.1 | nM | IC50 | J Med Chem (2004) 47: 6401-9 [PMID:15566309] |
ChEMBL | Tested for inhibition of [3H]cocaine binding to rat striatal P2 membranes | B | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (1994) 37: 2249-2252 [PMID:8035432] |
ChEMBL | Compound was evaluated for inhibition of specifically bound [3H]- cocaine (2.7 nM) against Dopamine transporter in cynomolgus monkeys | B | 7.17 | pIC50 | 67.8 | nM | IC50 | J Med Chem (1991) 34: 1728-1731 [PMID:2033595] |
ChEMBL | Inhibition of [125I]RTI-55 cocaine binding to the dopamine transporter. | B | 7.18 | pIC50 | 66 | nM | IC50 | J Med Chem (1992) 35: 969-981 [PMID:1552510] |
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] | ||||||||
ChEMBL | Tested for affinity by radioligand [3H]-TCP displacement from phencyclidine binding site (PCP) in rat homogenates | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 4075-4081 [PMID:8258830] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of human Potassium channel HERG expressed in mammalian cells | B | 5.14 | pIC50 | 7244.36 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512] |
ChEMBL | Inhibitory concentration against potassium channel HERG | B | 5.14 | pIC50 | 7244.36 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273] |
ChEMBL | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique | B | 5.14 | pIC50 | 7244.36 | nM | IC50 | Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342] |
ChEMBL | Inhibition of partially open human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) | F | 5.24 | pIC50 | 5754.4 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831] |
ChEMBL | Inhibition of human ERG in MCF7 cells | B | 5.24 | pIC50 | 5754.4 | nM | IC50 | Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341] |
ChEMBL | K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 | F | 8.36 | pIC50 | 4.4 | nM | IC50 | J Med Chem (2002) 45: 3844-3853 [PMID:12190308] |
M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
ChEMBL | Binding affinity at muscarinic M1 receptor in rat brain by [3H]pirenzepine displacement. | B | 4.21 | pKi | 61400 | nM | Ki | J Med Chem (2004) 47: 3388-3398 [PMID:15189035] |
ChEMBL | Displacement of [3H]pirenzepine from M1 receptor in Sprague-Dawley rat brain | B | 4.21 | pKi | 61400 | nM | Ki | J Med Chem (2006) 49: 6391-6399 [PMID:17034144] |
ChEMBL | Displacement of [3H]pirenzepine from muscarinic acetylcholine receptor M1 of rat brain membrane | B | 4.21 | pKi | 61397 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 3295-3298 [PMID:15149693] |
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
ChEMBL | Inhibition of [3H]mazindol binding to recombinant human NET expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis | B | 4.97 | pKi | 10700 | nM | Ki | J Med Chem (2017) 60: 3109-3123 [PMID:28319392] |
ChEMBL | Binding affinity against norepinephrine cloned human transporter using 40-80 pM [125I]RTI | B | 5.57 | pKi | 2700 | nM | Ki | J Med Chem (2000) 43: 4981-4992 [PMID:11150168] |
ChEMBL | Inhibition of [125I]RTI-55 binding to recombinant human NET expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis | B | 5.62 | pKi | 2410 | nM | Ki | J Med Chem (2017) 60: 3109-3123 [PMID:28319392] |
ChEMBL | Displacement of [125I]RTI-55 from human recombinant NET expressed in HEK293 cells by scintillation counting | B | 5.62 | pKi | 2377 | nM | Ki | Bioorg Med Chem (2009) 17: 6890-6897 [PMID:19740668] |
ChEMBL | Displacement of [125I]RTI-55 from human NET expressed in HEK293 cell membranes | B | 5.63 | pKi | 2357 | nM | Ki | J Med Chem (2018) 61: 9121-9131 [PMID:30240563] |
ChEMBL | Displacement of [125I]RTI-55 from human NET expressed in HEK293 cells | B | 5.67 | pKi | 2150 | nM | Ki | J Med Chem (2006) 49: 1420-1432 [PMID:16480278] |
ChEMBL | Displacement of [3H]nisoxetine from NET | B | 5.7 | pKi | 1990 | nM | Ki | J Med Chem (2005) 48: 7437-7444 [PMID:16279803] |
ChEMBL | Displacement of [3H]nisoxetine from human NET | B | 5.7 | pKi | 1990 | nM | Ki | J Med Chem (2006) 49: 4589-4594 [PMID:16854064] |
ChEMBL | Displacement of [3H]nisoxetine from NET | B | 5.7 | pKi | 1990 | nM | Ki | J Med Chem (2004) 47: 6401-6409 [PMID:15566309] |
ChEMBL | Displacement of [3H]nisoxetine from norepinephrine transporter | B | 5.7 | pKi | 1990 | nM | Ki | Bioorg Med Chem (2008) 16: 5529-5535 [PMID:18434164] |
ChEMBL | Displacement of [3H]nisoxetine from NET | B | 5.7 | pKi | 1990 | nM | Ki | Bioorg Med Chem (2009) 17: 5126-5132 [PMID:19523837] |
ChEMBL | Displacement of [125I]RTI-55 from human Norepinephrine transporter expressed in HEK cells | B | 5.71 | pKi | 1940 | nM | Ki | J Med Chem (2002) 45: 4097-4109 [PMID:12213053] |
ChEMBL | Binding affinity at the norepinephrine transporter was measured using [125I]RTI-55 as a radioligand | B | 5.75 | pKi | 1770 | nM | Ki | J Med Chem (2000) 43: 205-213 [PMID:10649976] |
ChEMBL | Inhibition of [125I]RTI-55 binding to norepinephrine transporter (NET) expressed in HEK cells | B | 5.75 | pKi | 1770 | nM | Ki | J Med Chem (1999) 42: 3647-3656 [PMID:10479296] |
ChEMBL | Compound was evaluated for binding affinity using [125I]RTI-55 as a radioligand in HEK-hNET cells expressing human norepinephrine transporter | B | 5.76 | pKi | 1740 | nM | Ki | J Med Chem (2000) 43: 2064-2071 [PMID:10821718] |
ChEMBL | Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay | B | 5.9 | pKi | 1257 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445] |
ChEMBL | Displacement of [125I]RTI55 from human NET expressed in HEK cells | B | 5.95 | pKi | 1116 | nM | Ki | Bioorg Med Chem (2009) 17: 2047-2068 [PMID:19201198] |
ChEMBL | Displacement of [125I]RTI-55 from human recombinant NET expressed in HEK293 cells by scintillation counting | B | 5.95 | pKi | 1115 | nM | Ki | J Med Chem (2009) 52: 1530-1539 [PMID:19256502] |
ChEMBL | Displacement of [125I]RTI55 from human recombinant NET expressed in HEK293 cells | B | 5.95 | pKi | 1115 | nM | Ki | Bioorg Med Chem (2009) 17: 337-343 [PMID:19014888] |
ChEMBL | Displacement of [125I]RTI55 from human NET expressed in COS1 cell membrane | B | 6.05 | pKi | 887 | nM | Ki | Bioorg Med Chem (2007) 15: 4159-4174 [PMID:17446076] |
ChEMBL | Displacement of [125I]RTI55 from cloned human NET expressed in HEK293 cells | B | 6.08 | pKi | 830 | nM | Ki | J Med Chem (2009) 52: 6768-6781 [PMID:19821577] |
ChEMBL | Compound was tested for inhibition of [125I]-RTI-55 binding to norepinephrine transporter HEK cells | B | 6.08 | pKi | 830 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2151-2154 [PMID:12798324] |
ChEMBL | Displacement of [125I]RT155 binding in HEK cells expressing human NET | B | 6.19 | pKi | 645 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 4133-4137 [PMID:14592523] |
ChEMBL | Displacement of [125I]RTI-55 from human NET expressing HEK293 cells | B | 6.3 | pKi | 500 | nM | Ki | J Med Chem (2007) 50: 219-232 [PMID:17228864] |
ChEMBL | Compound was evaluated for inhibition of [3H]NE uptake in HEK-hNET cells expressing Human norepinephrine transporter | B | 6.58 | pKi | 264 | nM | Ki | J Med Chem (2000) 43: 2064-2071 [PMID:10821718] |
ChEMBL | Inhibition of reuptake of [3H]-NE (20 nM) by norepinephrine transporter | B | 6.72 | pKi | 190 | nM | Ki | J Med Chem (2000) 43: 4981-4992 [PMID:11150168] |
ChEMBL | Inhibition of [3H]DA uptake in human NET expressed in COS1 cell membrane | F | 6.74 | pKi | 182 | nM | Ki | Bioorg Med Chem (2007) 15: 4159-4174 [PMID:17446076] |
ChEMBL | Inhibition of [3H]-NE uptake evaluated at the monoamine transporter (NET) | B | 6.97 | pKi | 108 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 513-517 [PMID:12565962] |
ChEMBL | Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay | B | 5.2 | pIC50 | 6309.57 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445] |
ChEMBL | Displacement of [3H]nisoxetine from NET | B | 5.48 | pIC50 | 3300 | nM | IC50 | J Med Chem (2005) 48: 7437-7444 [PMID:16279803] |
ChEMBL | Displacement of [3H]nisoxetine from NET | B | 5.48 | pIC50 | 3300 | nM | IC50 | J Med Chem (2004) 47: 6401-6409 [PMID:15566309] |
ChEMBL | Displacement of [3H]nisoxetine from human NET | B | 5.48 | pIC50 | 3300 | nM | IC50 | J Med Chem (2006) 49: 4589-4594 [PMID:16854064] |
ChEMBL | Displacement of [125I]RTI-55 from human Norepinephrine transporter expressed in HEK293 cells | B | 5.52 | pIC50 | 2990 | nM | IC50 | J Med Chem (2005) 48: 2876-2881 [PMID:15828826] |
ChEMBL | Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells | B | 5.72 | pIC50 | 1900 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 4133-4140 [PMID:17846138] |
ChEMBL | Inhibition of [3H]norepinephrine reuptake at human NET expressed in HEK cells | B | 5.89 | pIC50 | 1281 | nM | IC50 | Bioorg Med Chem (2009) 17: 2047-2068 [PMID:19201198] |
ChEMBL | Inhibition of rat NET-mediated norepinephrine uptake in CHO cells | B | 6.05 | pIC50 | 900 | nM | IC50 | J Med Chem (2006) 49: 4048-4051 [PMID:16821765] |
ChEMBL | Displacement of [3H]norepinephrine from human recombinant NET expressed in HEK293 cells by scintillation counting | B | 6.08 | pIC50 | 835 | nM | IC50 | J Med Chem (2009) 52: 1530-1539 [PMID:19256502] |
ChEMBL | Inhibition of [3H]NE from human recombinant NET expressed in HEK293 cells | B | 6.08 | pIC50 | 835 | nM | IC50 | Bioorg Med Chem (2009) 17: 337-343 [PMID:19014888] |
ChEMBL | Inhibition of [3H]norepinephrine uptake in HEK293 cells expressing human norepinephrine transporter | F | 6.34 | pIC50 | 462 | nM | IC50 | J Med Chem (2005) 48: 2876-2881 [PMID:15828826] |
ChEMBL | Compound was tested for inhibition of [3H]NE binding to norepinephrine transporter HEK cells | B | 6.41 | pIC50 | 385 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2151-2154 [PMID:12798324] |
ChEMBL | Inhibition of [3H]norepinephrine reuptake at human NET expressed in HEK293 cells | B | 6.41 | pIC50 | 385 | nM | IC50 | J Med Chem (2009) 52: 6768-6781 [PMID:19821577] |
ChEMBL | Inhibition of [3H] norepinephrine uptake into human NET expressed in HEK293 cells | F | 6.42 | pIC50 | 378 | nM | IC50 | J Med Chem (2006) 49: 1420-1432 [PMID:16480278] |
ChEMBL | Inhibition of NE uptake in HEK cells expressing human noradrenaline transporter (hNET) | F | 6.63 | pIC50 | 233 | nM | IC50 | J Med Chem (2002) 45: 4097-4109 [PMID:12213053] |
ChEMBL | Inhibition of [3H]NE reuptake at human NET expressed in HEK cells | B | 6.63 | pIC50 | 232 | nM | IC50 | Bioorg Med Chem (2009) 17: 6890-6897 [PMID:19740668] |
ChEMBL | Inhibition of [3H]NE reuptake by human norepinephrine transporter expressed in HEK293 cells | B | 6.64 | pIC50 | 230 | nM | IC50 | J Med Chem (2000) 43: 205-213 [PMID:10649976] |
ChEMBL | Inhibition of [3H]- NE uptake in HEK cells expressing norepinephrine transporter | F | 6.64 | pIC50 | 230 | nM | IC50 | J Med Chem (1999) 42: 3647-3656 [PMID:10479296] |
ChEMBL | Inhibition of recombinant human NET expressed in HEK293 cell membranes assessed as reduction in [3H]-norepinephrine uptake incubated for 22 mins by micro beta scintillation counting analysis | B | 6.66 | pIC50 | 221 | nM | IC50 | J Med Chem (2017) 60: 3109-3123 [PMID:28319392] |
ChEMBL | Inhibition of [3H]NE uptake into human NET expressing HEK293 cells | B | 6.68 | pIC50 | 210 | nM | IC50 | J Med Chem (2007) 50: 219-232 [PMID:17228864] |
ChEMBL | Inhibition of [3H]norepinephrine uptake in HEK cells expressing human NET | B | 6.72 | pIC50 | 192 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4133-4137 [PMID:14592523] |
ChEMBL | The compound was tested for inhibition of [3H]norepinephrine uptake in HEK cells by expressing cDNA for human norepinephrine transporter | B | 6.73 | pIC50 | 186 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 297-300 [PMID:10698458] |
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 | 4.52 | pKi | >30000 | nM | Ki | J Med Chem (1996) 39: 543-548 [PMID:8558525] |
ChEMBL | Displacement of [3H]nisoxetine from norepinephrine transporter of rat cerebral cortex | B | 5.48 | pKi | 3320 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1131-1133 [PMID:15686927] |
ChEMBL | Displacement of [3H]-nisoxatine from norepinephrine transporter of rat brain membrane | B | 5.48 | pKi | 3302 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 3295-3298 [PMID:15149693] |
ChEMBL | Displacement of [3H]nisoxetine from NET in Sprague-Dawley rat brain | B | 5.48 | pKi | 3300 | nM | Ki | J Med Chem (2006) 49: 6391-6399 [PMID:17034144] |
ChEMBL | Displacement of [3H]nisoxetine from norepinephrine transporter (NET) of rat brain | B | 5.48 | pKi | 3300 | nM | Ki | J Med Chem (2004) 47: 3388-3398 [PMID:15189035] |
ChEMBL | The compound was tested for binding affinity nisoxatine ligand | B | 5.48 | pKi | 3300 | nM | Ki | J Med Chem (1999) 42: 4446-4455 [PMID:10543888] |
ChEMBL | Inhibition of [3H]nisoxetine binding at norepinephrine transporter was determined | B | 5.7 | pKi | 2000 | nM | Ki | J Med Chem (2003) 46: 1775-1794 [PMID:12723940] |
ChEMBL | Binding affinity towards norepinephrine transporter was determined using [3H]nisoxetine radioligand. | B | 5.7 | pKi | 1990 | nM | Ki | J Med Chem (2004) 47: 296-302 [PMID:14711303] |
ChEMBL | Inhibition of 0.5 nM [3H]nisoxetine binding to Norepinephrine transporter | B | 5.72 | pKi | 1900 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2445-2447 [PMID:11078197] |
ChEMBL | Displacement of [3H]nisoxetine from norepinephrine transporter (NET) of rat cerebral cortex | B | 5.72 | pKi | 1900 | nM | Ki | J Med Chem (2005) 48: 3852-3857 [PMID:15916437] |
ChEMBL | Inhibition of [3H]NE uptake at Norepinephrine transporter in rat parietal/occipital cortex was determined | B | 6.72 | pKi | 190 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1113-1118 [PMID:11354356] |
ChEMBL | Inhibition of [3H]NE binding to norepinephrine transporter of rat brain synaptosomes | B | 6.73 | pKi | 186 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1681-1686 [PMID:10937724] |
ChEMBL | Inhibition of [3H]NE uptake by rat frontal cortex Norepinephrine transporter | B | 6.79 | pKi | 160.55 | nM | Ki | J Med Chem (1995) 38: 379-388 [PMID:7830281] |
ChEMBL | Displacement of [3H]NE from Norepinephrine transporter of rat brain | B | 6.97 | pKi | 108 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2079-2083 [PMID:11514143] |
ChEMBL | Inhibition of [3H]NE Uptake in rat parietal/occipital cortex | B | 6.97 | pKi | 108 | nM | Ki | J Med Chem (2000) 43: 351-360 [PMID:10669562] |
ChEMBL | Ability to inhibit [3H]NE reuptake at norepinephrine transporter from rat brain | B | 6.97 | pKi | 108 | nM | Ki | J Med Chem (2003) 46: 1997-2007 [PMID:12723962] |
ChEMBL | Inhibition of [3H]NE uptake by Norepinephrine transporter of rat occipital cortex synaptosomes | B | 6.97 | pKi | 108 | nM | Ki | J Med Chem (2000) 43: 1215-1222 [PMID:10737754] |
ChEMBL | Ability to inhibit high affinity uptake of norepinephrine transporter into the nerve endings of rat synaptosomes using [3H]NE as a radioligand | B | 6.97 | pKi | 108 | nM | Ki | J Med Chem (2001) 44: 1615-1622 [PMID:11334571] |
ChEMBL | Ability to inhibit reuptake of norepinephrine ([3H]NE) at norepinephrine transporter of rat parietal/occipital region | B | 6.97 | pKi | 108 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 3565-3569 [PMID:14505672] |
ChEMBL | Inhibition of reuptake of [3H]-NE at Norepinephrine transporter | B | 6.97 | pKi | 108 | nM | Ki | J Med Chem (2000) 43: 2064-2071 [PMID:10821718] |
ChEMBL | Compound was tested for its ability to inhibit high-affinity uptake of [3H]NE into parietal and occipital cortex in rat | B | 6.97 | pKi | 108 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1443-1446 [PMID:10888328] |
ChEMBL | Inhibition of high affinity uptake of [3H]NE by norepinephrine transporter in nerve endings obtained from rat brain. | B | 6.97 | pKi | 108 | nM | Ki | J Med Chem (2002) 45: 3161-3170 [PMID:12109901] |
ChEMBL | Ability to inhibit high affinity uptake of [3H]NE at Norepinephrine transporter (NET) using rat brain parietal/occipital cortex | B | 6.97 | pKi | 108 | nM | Ki | J Med Chem (2004) 47: 3009-3018 [PMID:15163183] |
ChEMBL | Inhibition of [3H]-NE reuptake at Norepinephrine transporter in rat parietal/occipital cortex | B | 6.97 | pKi | 108 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 993-995 [PMID:11909701] |
ChEMBL | Ability to inhibit high affinity reuptake of [3H]-NE (Norepinephrine transporter) into nerve ending synaptosomes prepared from brain regions | B | 6.97 | pKi | 108 | nM | Ki | J Med Chem (2002) 45: 1930-1941 [PMID:11960503] |
ChEMBL | Inhibition of high affinity uptake by the norepinephrine transporter from rat synaptosomal nerve endings by using [3H]NE as radioligand | B | 6.97 | pKi | 108 | nM | Ki | J Med Chem (2004) 47: 5821-5824 [PMID:15537337] |
ChEMBL | Inhibition of [3H]mazindol binding to Norepinephrine transporter | B | 5.42 | pIC50 | 3825 | nM | IC50 | J Med Chem (1992) 35: 2497-2500 [PMID:1619622] |
ChEMBL | Inhibition of binding of [3H]nisoxetine to (NET) norepinephrine transporter in rat striatum | B | 5.45 | pIC50 | 3530 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1591-1595 [PMID:12699762] |
ChEMBL | Binding affinity towards norepinephrine transporter in rat striatum using [3H]nisoxetine as radioligand | B | 5.45 | pIC50 | 3530 | nM | IC50 | J Med Chem (2003) 46: 1220-1228 [PMID:12646032] |
ChEMBL | Inhibition of [3H]nisoxetine binding to norepinephrine transporter of rat cerebral cortex | B | 5.45 | pIC50 | 3530 | nM | IC50 | J Med Chem (2004) 47: 5101-5113 [PMID:15456254] |
ChEMBL | Affinity at norepinephrine transporter (NET) in rat striatum, using [3H]- nisoxatine as radioligand | B | 5.45 | pIC50 | 3530 | nM | IC50 | J Med Chem (2001) 44: 937-948 [PMID:11300876] |
ChEMBL | Binding affinity at the norepinephrine transporter in rat striatum by [3H]nisoxetine displacement. | B | 5.45 | pIC50 | 3530 | nM | IC50 | J Med Chem (2003) 46: 2205-2215 [PMID:12747792] |
ChEMBL | Inhibition of binding of [3H]- nisoxatine to Norepinephrine transporter (NET) of rat cerebral cortex. | B | 5.45 | pIC50 | 3530 | nM | IC50 | J Med Chem (2002) 45: 654-662 [PMID:11806716] |
ChEMBL | Binding affinity was evaluated by measuring inhibiting the binding of [3H]nisoxetine to Norepinephrine transporter in rat brain tissue | B | 5.45 | pIC50 | 3520 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2337-2340 [PMID:11527726] |
ChEMBL | Inhibition of [3H]nisoxetine binding to rat cerebral cortex norepinephrine transporter | B | 5.48 | pIC50 | 3300 | nM | IC50 | J Med Chem (2005) 48: 3852-3857 [PMID:15916437] |
ChEMBL | Inhibition of norepinephrine transporter (NET) determined using [3H]nisoxetine radioligand. | B | 5.48 | pIC50 | 3300 | nM | IC50 | J Med Chem (2004) 47: 296-302 [PMID:14711303] |
ChEMBL | In vitro inhibitory activity against radioligand [3H]-nisoxatine binding to norepinephrine transporter (NET) in rat cortical tissue | B | 5.48 | pIC50 | 3300 | nM | IC50 | J Med Chem (1997) 40: 3861-3864 [PMID:9397165] |
ChEMBL | Inhibition of [3H]nisoxetine binding at norepinephrine transporter was determined | B | 5.48 | pIC50 | 3300 | nM | IC50 | J Med Chem (2003) 46: 1775-1794 [PMID:12723940] |
ChEMBL | Norepinephrine transporter activity was determined by the ability of compound to inhibit the neurotransmitter norepinephrine-NE reuptake system using [3H]norepinephrine as radioligand | B | 5.48 | pIC50 | 3300 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 2559-2564 |
ChEMBL | Inhibition of 0.5 nM [3H]nisoxetine binding toNorepinephrine transporter | B | 5.48 | pIC50 | 3300 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2445-2447 [PMID:11078197] |
ChEMBL | Inhibitory activity against radioligand [3H]nisoxetine binding at the norepinephrine transporter | B | 5.48 | pIC50 | 3300 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 3689-3692 [PMID:9934496] |
ChEMBL | Inhibitory activity against Norepinephrine transporter using 0.5 nM [3H]-radioligand | B | 5.48 | pIC50 | 3300 | nM | IC50 | J Med Chem (1997) 40: 1247-1251 [PMID:9111298] |
ChEMBL | Selectivity for the norepinephrine transporter using [3H]nisoxetine binding assay | B | 5.48 | pIC50 | 3300 | nM | IC50 | J Med Chem (1999) 42: 4836-4843 [PMID:10579846] |
ChEMBL | Binding affinity at the Norepinephrine transporter in rat frontal cortex by inhibition of 0.5 nM [3H]nisoxetine binding | B | 5.48 | pIC50 | 3298 | nM | IC50 | J Med Chem (1995) 38: 379-388 [PMID:7830281] |
ChEMBL | Inhibition of [3H]nisoxetine binding to norepinephrine (NE) transporter | B | 5.48 | pIC50 | 3298 | nM | IC50 | J Med Chem (1994) 37: 1220-1223 [PMID:8164265] |
ChEMBL | Binding affinity towards Norepinephrine transporter was determined using NE[3H]Nisoxetine as radioligand | B | 5.48 | pIC50 | 3298 | nM | IC50 | J Med Chem (1995) 38: 3451-3453 [PMID:7658431] |
ChEMBL | Binding potency for Norepinephrine transporter using [3H]NE | B | 5.48 | pIC50 | 3298 | nM | IC50 | J Med Chem (1996) 39: 4139-4141 [PMID:8863789] |
ChEMBL | Inhibition of [3H]nisoxetine binding to the norepinephrine transporter in rat midbrain. | B | 5.48 | pIC50 | 3298 | nM | IC50 | J Med Chem (1996) 39: 4027-4035 [PMID:8831768] |
ChEMBL | Inhibition of norepinephrine Transporter Affinity against rat whole brain using [3H]nisoxetine radioligand | B | 5.6 | pIC50 | 2500 | nM | IC50 | J Med Chem (1998) 41: 2380-2389 [PMID:9632371] |
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
ChEMBL | Displacement of [125I]RTI55 from human SERT expressed in COS1 cell membrane | B | 6.02 | pKi | 965 | nM | Ki | Bioorg Med Chem (2007) 15: 4159-4174 [PMID:17446076] |
ChEMBL | Inhibition of [3H]5-HT uptake at human SERT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay | B | 6.09 | pKi | 818 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445] |
ChEMBL | Inhibition of [125I]RTI-55 binding to recombinant human SERT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis | B | 6.18 | pKi | 657 | nM | Ki | J Med Chem (2017) 60: 3109-3123 [PMID:28319392] |
ChEMBL | Displacement of [125I]RTI-55 from human SERT expressed in HEK293 cell membranes | B | 6.2 | pKi | 632 | nM | Ki | J Med Chem (2018) 61: 9121-9131 [PMID:30240563] |
ChEMBL | Displacement of [125I]RTI55 from cloned human SERT expressed in HEK293 cells | B | 6.22 | pKi | 601 | nM | Ki | J Med Chem (2009) 52: 6768-6781 [PMID:19821577] |
ChEMBL | Compound was tested for inhibition of [125I]RTI-55 binding to Serotonin transporter in HEK cells | B | 6.22 | pKi | 601 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2151-2154 [PMID:12798324] |
ChEMBL | Displacement of [125I]RTI-55 from human recombinant SERT expressed in HEK293 cells | B | 6.28 | pKi | 525 | nM | Ki | Bioorg Med Chem (2009) 17: 6890-6897 [PMID:19740668] |
ChEMBL | Inhibition of [3H]SER uptake in human SERT expressed in COS1 cell membrane | F | 6.28 | pKi | 524 | nM | Ki | Bioorg Med Chem (2007) 15: 4159-4174 [PMID:17446076] |
ChEMBL | Binding affinity against cloned serotonin human transporter using 40-80 PM [125I]RTI | B | 6.3 | pKi | 500 | nM | Ki | J Med Chem (2000) 43: 4981-4992 [PMID:11150168] |
ChEMBL | Binding affinity for serotonin transporter using [125I]RTI-55 | B | 6.41 | pKi | 390 | nM | Ki | J Med Chem (2000) 43: 205-213 [PMID:10649976] |
ChEMBL | Inhibition of [125I]RTI-55 binding to serotonin transporter (SERT) expressed in HEK cells | B | 6.41 | pKi | 387 | nM | Ki | J Med Chem (1999) 42: 3647-3656 [PMID:10479296] |
ChEMBL | Displacement of [125I]RTI-55 from human SERT expressed in HEK293 cells | B | 6.45 | pKi | 358 | nM | Ki | J Med Chem (2006) 49: 1420-1432 [PMID:16480278] |
ChEMBL | Compound was evaluated for binding affinity using [125I]RTI-55 as a radioligand in HEK-hSERT cells expressing human serotonin transporter | B | 6.46 | pKi | 343 | nM | Ki | J Med Chem (2000) 43: 2064-2071 [PMID:10821718] |
ChEMBL | Displacement of [125I]RTI-55 from human SERT expressing HEK293 cells | B | 6.47 | pKi | 340 | nM | Ki | J Med Chem (2007) 50: 219-232 [PMID:17228864] |
ChEMBL | Displacement of [125I]- RTI-55 from Serotonin transporter expressed in HEK cells | B | 6.48 | pKi | 328 | nM | Ki | J Med Chem (2002) 45: 4097-4109 [PMID:12213053] |
ChEMBL | Inhibition of reuptake of [3H]5-HT (20 nM) by serotonin transporter | B | 6.51 | pKi | 310 | nM | Ki | J Med Chem (2000) 43: 4981-4992 [PMID:11150168] |
ChEMBL | Compound was evaluated for inhibition of [3H]5-HT uptake in HEK-hSERT cells expressing Human serotonin transporter | B | 6.52 | pKi | 301 | nM | Ki | J Med Chem (2000) 43: 2064-2071 [PMID:10821718] |
ChEMBL | Displacement of [125I]RT155 binding in HEK cells expressing human SERT | B | 6.53 | pKi | 297 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 4133-4137 [PMID:14592523] |
ChEMBL | Displacement of [125I]RTI55 from human recombinant SERT expressed in HEK293 cells | B | 6.56 | pKi | 276 | nM | Ki | Bioorg Med Chem (2009) 17: 337-343 [PMID:19014888] |
ChEMBL | Displacement of [125I]RTI-55 from human recombinant SERT expressed in HEK293 cells by scintillation counting | B | 6.56 | pKi | 276 | nM | Ki | J Med Chem (2009) 52: 1530-1539 [PMID:19256502] |
ChEMBL | Displacement of [125I]RTI55 from human SERT expressed in HEK cells | B | 6.56 | pKi | 276 | nM | Ki | Bioorg Med Chem (2009) 17: 2047-2068 [PMID:19201198] |
ChEMBL | Inhibition of [3H]mazindol binding to recombinant human SERT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis | B | 6.64 | pKi | 229 | nM | Ki | J Med Chem (2017) 60: 3109-3123 [PMID:28319392] |
ChEMBL | Inhibition of [3H]-5-HT uptake evaluated at the Serotonin transporter | B | 6.81 | pKi | 155 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 513-517 [PMID:12565962] |
ChEMBL | Binding affinity at SERT | B | 6.89 | pKi | 129 | nM | Ki | J Med Chem (2008) 51: 2795-2806 [PMID:18393401] |
ChEMBL | Displacement of [3H]paroxetine from 5-HTT | B | 7.02 | pKi | 95 | nM | Ki | Bioorg Med Chem (2009) 17: 5126-5132 [PMID:19523837] |
ChEMBL | Displacement of [3H]paroxetine from serotonin transporter | B | 7.02 | pKi | 95 | nM | Ki | Bioorg Med Chem (2008) 16: 5529-5535 [PMID:18434164] |
ChEMBL | Displacement of [3H]paroxetine from 5HTT | B | 7.35 | pKi | 45 | nM | Ki | J Med Chem (2005) 48: 7437-7444 [PMID:16279803] |
ChEMBL | Displacement of [3H]paroxetine from 5HTT | B | 7.35 | pKi | 45 | nM | Ki | J Med Chem (2004) 47: 6401-6409 [PMID:15566309] |
ChEMBL | Displacement of [3H]paroxetine from human 5HTT | B | 7.35 | pKi | 45 | nM | Ki | J Med Chem (2006) 49: 4589-4594 [PMID:16854064] |
ChEMBL | Inhibition of [3H]5-HT uptake at human SERT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay | B | 5.62 | pIC50 | 2398.83 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445] |
ChEMBL | Displacement of [3H]paroxetine from 5HTT | B | 5.98 | pIC50 | 1050 | nM | IC50 | J Med Chem (2004) 47: 6401-6409 [PMID:15566309] |
ChEMBL | Displacement of [3H]paroxetine from 5HTT | B | 5.98 | pIC50 | 1050 | nM | IC50 | J Med Chem (2005) 48: 7437-7444 [PMID:16279803] |
ChEMBL | Displacement of [3H]paroxetine from human 5HTT | B | 5.98 | pIC50 | 1050 | nM | IC50 | J Med Chem (2006) 49: 4589-4594 [PMID:16854064] |
ChEMBL | Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK cells | B | 6.19 | pIC50 | 642 | nM | IC50 | Bioorg Med Chem (2009) 17: 2047-2068 [PMID:19201198] |
ChEMBL | Displacement of [3H]citalopram from human SERT expressed in HEK293 cell membrane | B | 6.27 | pIC50 | 540 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 48-51 [PMID:21146984] |
ChEMBL | Inhibition of [3H] serotonin uptake into human SERT expressed in HEK293 cells | F | 6.31 | pIC50 | 494 | nM | IC50 | J Med Chem (2006) 49: 1420-1432 [PMID:16480278] |
ChEMBL | Displacement of [125I]RTI-55 from human Serotonin transporter expressed in HEK293 cells | B | 6.36 | pIC50 | 433 | nM | IC50 | J Med Chem (2005) 48: 2876-2881 [PMID:15828826] |
ChEMBL | Inhibition of [3H]5HT from human recombinant SERT expressed in HEK293 cells | B | 6.38 | pIC50 | 416 | nM | IC50 | Bioorg Med Chem (2009) 17: 337-343 [PMID:19014888] |
ChEMBL | Displacement of [3H]serotonin from human recombinant SERT expressed in HEK293 cells by scintillation counting | B | 6.38 | pIC50 | 416 | nM | IC50 | J Med Chem (2009) 52: 1530-1539 [PMID:19256502] |
ChEMBL | The compound was tested for inhibition of [3H]-5-hydroxy tryptamine uptake in HEK cells by expressing cDNA for human tryptamine transporter | B | 6.38 | pIC50 | 413 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 297-300 [PMID:10698458] |
ChEMBL | Inhibition of [3H]5-HT reuptake in HEK293 cells expressing human serotonin transporter | B | 6.47 | pIC50 | 340 | nM | IC50 | J Med Chem (2000) 43: 205-213 [PMID:10649976] |
ChEMBL | Inhibition of [3H]5HT reuptake at human SERT expressed in HEK293 cells | B | 6.47 | pIC50 | 338 | nM | IC50 | Bioorg Med Chem (2009) 17: 6890-6897 [PMID:19740668] |
ChEMBL | Inhibition of 5-HT uptake in HEK cells expressing human serotonin transporter (hSERT) | F | 6.47 | pIC50 | 338 | nM | IC50 | J Med Chem (2002) 45: 4097-4109 [PMID:12213053] |
ChEMBL | Inhibition of [3H]- 5-HT uptake in HEK cells expressing serotonin transporter | F | 6.47 | pIC50 | 336 | nM | IC50 | J Med Chem (1999) 42: 3647-3656 [PMID:10479296] |
ChEMBL | Inhibition of [3H]5-HT uptake in HEK cells expressing human SERT | B | 6.49 | pIC50 | 325 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4133-4137 [PMID:14592523] |
ChEMBL | Compound was tested for inhibition of [3H]5-HT binding to Serotonin transporter in HEK cells | B | 6.5 | pIC50 | 318 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2151-2154 [PMID:12798324] |
ChEMBL | Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK293 cells | B | 6.5 | pIC50 | 318 | nM | IC50 | J Med Chem (2009) 52: 6768-6781 [PMID:19821577] |
ChEMBL | Inhibition of [3H]5HT uptake in SERT | B | 6.52 | pIC50 | 304 | nM | IC50 | J Med Chem (2008) 51: 2795-2806 [PMID:18393401] |
ChEMBL | Inhibition of [3H]5-HT uptake in HEK293 cells expressing human serotonin transporter | F | 6.54 | pIC50 | 289 | nM | IC50 | J Med Chem (2005) 48: 2876-2881 [PMID:15828826] |
ChEMBL | Inhibition of recombinant human SERT expressed in HEK293 cell membranes assessed as reduction in [3H]5-HT uptake incubated for 22 mins by micro beta scintillation counting analysis | B | 6.56 | pIC50 | 277 | nM | IC50 | J Med Chem (2017) 60: 3109-3123 [PMID:28319392] |
ChEMBL | Inhibition of [3H]citalopram binding to serotonin transporter (SERT) of cynomolgus monkey caudate-putamen | B | 6.57 | pIC50 | 270 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 857-862 [PMID:10206550] |
ChEMBL | Ability to inhibit [3H]citalopram binding to serotonin transporter in cynomolgus monkey striatum | B | 6.57 | pIC50 | 270 | nM | IC50 | J Med Chem (1993) 36: 855-862 [PMID:8464040] |
ChEMBL | Inhibition of [3H]5-HT uptake into human SERT expressing HEK293 cells | B | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (2007) 50: 219-232 [PMID:17228864] |
ChEMBL | Inhibition of [3H]5HT uptake at human SERT expressed in HEK293 cells | B | 6.74 | pIC50 | 180 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 4133-4140 [PMID:17846138] |
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
ChEMBL | In vitro binding affinity towards serotonin transporter in rat cerebral cortical homogenates by [3H]paroxetine displacement. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1996) 39: 543-548 [PMID:8558525] |
ChEMBL | Displacement of [3H]paroxetine from serotonin transporter of rat cerebral cortex | B | 5.98 | pKi | 1050 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1131-1133 [PMID:15686927] |
ChEMBL | Inhibition of [3H]-5-HT binding to serotonin transporter of rat brain synaptosomes | B | 6.38 | pKi | 413 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1681-1686 [PMID:10937724] |
ChEMBL | Displacement of [3H]-citalopram from serotonin transporter of rat brain membrane | B | 6.53 | pKi | 293 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 3295-3298 [PMID:15149693] |
ChEMBL | Displacement of [3H]citalopram from SERT in Sprague-Dawley rat brain membranes | B | 6.54 | pKi | 286 | nM | Ki | ACS Med Chem Lett (2011) 2: 48-52 [PMID:21344069] |
ChEMBL | Displacement of [3H]citalopram from SERT in rat brain | B | 6.54 | pKi | 286 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6865-6868 [PMID:19896846] |
ChEMBL | Binding affinity at serotonin transporter in rat brain by [3H]-citalopram displacement. | B | 6.54 | pKi | 286 | nM | Ki | J Med Chem (2004) 47: 3388-3398 [PMID:15189035] |
ChEMBL | Displacement of [3H]citalopram from SERT in Sprague-Dawley rat brain | B | 6.54 | pKi | 286 | nM | Ki | J Med Chem (2006) 49: 6391-6399 [PMID:17034144] |
ChEMBL | Binding affinity against Serotonin transporter in male Sprague-Dawley rats using [3H]paroxetine ligand | B | 6.76 | pKi | 172 | nM | Ki | J Med Chem (1999) 42: 4446-4455 [PMID:10543888] |
ChEMBL | Inhibition of [3H]5-HT uptake at striatal nerve endings by serotonin transporter | B | 6.8 | pKi | 160 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 3325-3328 [PMID:10612593] |
ChEMBL | Inhibition of [3H]5-HT uptake at Serotonin transporter in rat mid brain | B | 6.8 | pKi | 160 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1113-1118 [PMID:11354356] |
ChEMBL | Compound was tested for its ability to inhibit high affinity uptake of [3H]5-HT into mid brain nerve endings (synaptosomes) in rat | B | 6.8 | pKi | 160 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1443-1446 [PMID:10888328] |
ChEMBL | Inhibition of high affinity uptake of [3H]5-HT by serotonin transporter in nerve endings obtained from rat brain. | B | 6.81 | pKi | 155 | nM | Ki | J Med Chem (2002) 45: 3161-3170 [PMID:12109901] |
ChEMBL | Inhibition of [3H]5-HT Uptake in rat mid brain. | B | 6.81 | pKi | 155 | nM | Ki | J Med Chem (2000) 43: 351-360 [PMID:10669562] |
ChEMBL | Ability to inhibit [3H]5-HT reuptake at serotonin transporter from rat brain | B | 6.81 | pKi | 155 | nM | Ki | J Med Chem (2003) 46: 1997-2007 [PMID:12723962] |
ChEMBL | Inhibition of [3H]5-HT uptake by Serotonin transporter of rat midbrain or parietal synaptosomes | B | 6.81 | pKi | 155 | nM | Ki | J Med Chem (2000) 43: 1215-1222 [PMID:10737754] |
ChEMBL | Inhibition of high affinity serotonin uptake into rat synaptosomes using [3H]5-HT | B | 6.81 | pKi | 155 | nM | Ki | J Med Chem (2001) 44: 1615-1622 [PMID:11334571] |
ChEMBL | Ability to inhibit reuptake of serotonin ([3H]5-HT) at serotonin transporter of rat midbrian | B | 6.81 | pKi | 155 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 3565-3569 [PMID:14505672] |
ChEMBL | Inhibition of reuptake of [3H]5-HT at serotonin transporter | B | 6.81 | pKi | 155 | nM | Ki | J Med Chem (2000) 43: 2064-2071 [PMID:10821718] |
ChEMBL | Displacement of [3H]5-HT from serotonin transporter of rat brain | B | 6.81 | pKi | 155 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2079-2083 [PMID:11514143] |
ChEMBL | Ability to inhibit high affinity uptake of [3H]-5-HT at Serotonin transporter (SERT) using rat midbrain | B | 6.81 | pKi | 155 | nM | Ki | J Med Chem (2004) 47: 3009-3018 [PMID:15163183] |
ChEMBL | Inhibition of [3H]5-HT reuptake at serotonin transporter in rat mid brain | B | 6.81 | pKi | 155 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 993-995 [PMID:11909701] |
ChEMBL | Binding affinity for Serotonin transporter was determined by [3H]5-HT (serotonin) uptake by striated synaptosomes | B | 6.81 | pKi | 155 | nM | Ki | J Med Chem (1998) 41: 4973-4982 [PMID:9836615] |
ChEMBL | Inhibition of high affinity re-uptake of [3H]5-HT (serotonin) into nerve ending synaptosomes | B | 6.81 | pKi | 155 | nM | Ki | J Med Chem (2002) 45: 1930-1941 [PMID:11960503] |
ChEMBL | Inhibition of high affinity uptake by the serotonin transporter (5-HT) from rat synaptosomal nerve endings by using [3H]5-HT as radioligand | B | 6.81 | pKi | 155 | nM | Ki | J Med Chem (2004) 47: 5821-5824 [PMID:15537337] |
ChEMBL | Inhibition of [125I]RTI-55 binding to Serotonin transporter of rat caudate membranes | B | 6.89 | pKi | 130 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2225-2228 [PMID:12127543] |
ChEMBL | Ratio of Ki value towards Serotonin transporter to that of dopamine transporter | B | 6.95 | pKi | 112.11 | nM | Ki | J Med Chem (1995) 38: 379-388 [PMID:7830281] |
ChEMBL | Inhibition of [3H]paroxetine binding at serotonin transporter was determined | B | 7.02 | pKi | 96 | nM | Ki | J Med Chem (2003) 46: 1775-1794 [PMID:12723940] |
ChEMBL | Inhibition of 0.2 nM [3H]paroxetine binding to Serotonin transporter | B | 7.02 | pKi | 95 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2445-2447 [PMID:11078197] |
ChEMBL | Displacement of [3H]paroxetine from serotonin transporter (5-HT) of rat cerebral cortex | B | 7.02 | pKi | 95 | nM | Ki | J Med Chem (2005) 48: 3852-3857 [PMID:15916437] |
ChEMBL | Binding affinity towards serotonin transporter 5-HTT was determined using [3H]paroxetine radioligand. | B | 7.35 | pKi | 45 | nM | Ki | J Med Chem (2004) 47: 296-302 [PMID:14711303] |
ChEMBL | Inhibition of [3H]paroxetine binding to Serotonin transporter | B | 5.98 | pIC50 | 1059 | nM | IC50 | J Med Chem (1992) 35: 2497-2500 [PMID:1619622] |
ChEMBL | Selectivity for the Serotonin transporter using [3H]paroxetine binding assay | B | 5.98 | pIC50 | 1050 | nM | IC50 | J Med Chem (1999) 42: 4836-4843 [PMID:10579846] |
ChEMBL | Inhibitory activity against Serotonin transporter using 0.2 nM [3H]paroxetine as radioligand | B | 5.98 | pIC50 | 1050 | nM | IC50 | J Med Chem (1997) 40: 1247-1251 [PMID:9111298] |
ChEMBL | Inhibitory concentration required to inhibit serotonin transporter 5-HTT was determined by using [3H]paroxetine radioligand | B | 5.98 | pIC50 | 1050 | nM | IC50 | J Med Chem (2004) 47: 296-302 [PMID:14711303] |
ChEMBL | In vitro inhibitory activity against radioligand [3H]paroxetine binding to serotonin transporter (5-HTT) in rat midbrain tissue | B | 5.98 | pIC50 | 1050 | nM | IC50 | J Med Chem (1997) 40: 3861-3864 [PMID:9397165] |
ChEMBL | Inhibition of [3H]paroxetine binding at serotonin transporter was determined | B | 5.98 | pIC50 | 1050 | nM | IC50 | J Med Chem (2003) 46: 1775-1794 [PMID:12723940] |
ChEMBL | Inhibition of 0.2 nM [3H]paroxetine binding to Serotonin transporter | B | 5.98 | pIC50 | 1050 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2445-2447 [PMID:11078197] |
ChEMBL | Inhibition of [3H]paroxetine binding to rat cortex serotonin transporter | B | 5.98 | pIC50 | 1050 | nM | IC50 | J Med Chem (2005) 48: 3852-3857 [PMID:15916437] |
ChEMBL | Inhibitory activity against radioligand [3H]paroxetine binding at the serotonin transporter | B | 5.98 | pIC50 | 1050 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 3689-3692 [PMID:9934496] |
ChEMBL | Compound was tested for its ability to inhibit the neurotransmitter serotonin-5-HT reuptake system using [3H]5-HT as radioligand | B | 5.98 | pIC50 | 1045 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 2559-2564 |
ChEMBL | Binding affinity towards Serotonin transporter was determined using 5-HT [3H]paroxetine as radioligand | B | 5.98 | pIC50 | 1045 | nM | IC50 | J Med Chem (1995) 38: 3451-3453 [PMID:7658431] |
ChEMBL | Binding affinity at the Serotonin transporter in rat midbrain by inhibition of 0.5 nM [3H]-paroxetine binding | B | 5.98 | pIC50 | 1045 | nM | IC50 | J Med Chem (1995) 38: 379-388 [PMID:7830281] |
ChEMBL | Inhibition of [3H]paroxetine binding to serotonin transporter in rat frontal cortex | B | 5.98 | pIC50 | 1045 | nM | IC50 | J Med Chem (1996) 39: 4027-4035 [PMID:8831768] |
ChEMBL | Inhibition of [3H]paroxetine binding to 5-hydroxytryptamine (5-HT) transporter | B | 5.98 | pIC50 | 1045 | nM | IC50 | J Med Chem (1994) 37: 1220-1223 [PMID:8164265] |
ChEMBL | Binding potency for Serotonin transporter using [3H]- paroxetine | B | 5.98 | pIC50 | 1045 | nM | IC50 | J Med Chem (1996) 39: 4139-4141 [PMID:8863789] |
ChEMBL | Binding affinity at serotonin transporter in rat striatum by [3H]citalopram displacement. | B | 6.13 | pIC50 | 737 | nM | IC50 | J Med Chem (2003) 46: 2205-2215 [PMID:12747792] |
ChEMBL | Inhibition of binding of [3H]citalopram to (SERT) serotonin transporter in rat striatum | B | 6.13 | pIC50 | 737 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1591-1595 [PMID:12699762] |
ChEMBL | Inhibition of [3H]citalopram binding to serotonin transporter of rat cerebral cortex | B | 6.13 | pIC50 | 737 | nM | IC50 | J Med Chem (2004) 47: 5101-5113 [PMID:15456254] |
ChEMBL | In vitro binding affinity at serotonin transporter in rat striatum by [3H]- citalopram displacement. | B | 6.13 | pIC50 | 737 | 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 | 6.13 | pIC50 | 737 | nM | IC50 | J Med Chem (2002) 45: 654-662 [PMID:11806716] |
ChEMBL | Binding affinity was evaluated by measuring inhibiting the binding of [3H]citalopram to Serotonin transporter in rat brain tissue | B | 6.13 | pIC50 | 737 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2337-2340 [PMID:11527726] |
ChEMBL | Binding affinity towards serotonin transporter in rat striatum using [3H]citalopram as radioligand | B | 6.13 | pIC50 | 737 | nM | IC50 | J Med Chem (2003) 46: 1220-1228 [PMID:12646032] |
ChEMBL | Inhibition of serotonin Transporter Affinity against rat whole brain using [3H]paroxetine as radioligand | B | 6.21 | pIC50 | 615 | nM | IC50 | J Med Chem (1998) 41: 2380-2389 [PMID:9632371] |
ChEMBL | Inhibition of rat SERT-mediated serotonin uptake in CHO cells | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2006) 49: 4048-4051 [PMID:16821765] |
ChEMBL | Inhibition of [3H]citalopram binding to Serotonin transporter (5-HTT) in rat cortical tissue. | B | 6.41 | pIC50 | 389 | nM | IC50 | J Med Chem (2003) 46: 1456-1464 [PMID:12672245] |
ChEMBL | Inhibition of [3H]5-HT reuptake at rat serotonin transporter | B | 6.52 | pIC50 | 304 | nM | IC50 | J Med Chem (1996) 39: 4704-4716 [PMID:8941383] |
ChEMBL | Compound was tested for binding affinity to Serotonin transporter sites in homogenates prepared from rat cortical membranes using [3H]paroxetine as radioligand | B | 6.68 | pIC50 | 207 | nM | IC50 | J Med Chem (1991) 34: 3144-3146 [PMID:1920365] |
ChEMBL | Inhibitory activity against Serotonin transporter was determined for [3H]5-HT (serotonin) uptake by striated synaptosomes | B | 6.77 | pIC50 | 168 | nM | IC50 | J Med Chem (1998) 41: 4973-4982 [PMID:9836615] |
ChEMBL | Displacement of [3H]paroxetine from Serotonin transporter of rat caudate putamen | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2005) 48: 3337-3343 [PMID:15857139] |
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
ChEMBL | Binding affinity against Sigma receptor type 1 was determined by the displacement of [3H]pentazocine radioligand | B | 5.05 | pKi | 8830 | nM | Ki | J Med Chem (2003) 46: 2589-2598 [PMID:12801223] |
Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380] | ||||||||
ChEMBL | Displacement of [3H]nisoxetine from NET in Sprague-Dawley rat brain membranes | B | 5.48 | pKi | 3300 | nM | Ki | ACS Med Chem Lett (2011) 2: 48-52 [PMID:21344069] |
ChEMBL | Displacement of [3H]nisoxetine from NET in rat brain | B | 5.5 | pKi | 3192 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6865-6868 [PMID:19896846] |
5-HT3AB in Human [GtoPdb: 378] | ||||||||
GtoPdb | - | - | 4.8 | pKi | - | - | - | Neuropharmacology (2001) 41: 282-4 [PMID:11489465] |
5-HT3A in Human [GtoPdb: 379] | ||||||||
GtoPdb | - | - | 5.4 | pKi | - | - | - |
Neuropharmacology (2001) 41: 282-4 [PMID:11489465]; Br J Pharmacol (1996) 118: 1237-45 [PMID:8818349] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]