cocaine [Ligand Id: 2286] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL370805 (RX-0041, RX0041, Cocaine, IDS-NC-004)
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
  • Norepinephrine transporter in Rat [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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  • 5-HT3AB in Human [GtoPdb: 378]
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  • 5-HT3A in Human [GtoPdb: 379]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 [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 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 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 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 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 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 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