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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 |