GBR12935 [Ligand Id: 4639] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL26320 (GBR-12935)
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL Inhibition of [125I]RTI-55 binding to dopamine transporter B 7.14 pKi 73 nM Ki J Med Chem (2000) 43: 205-213 [PMID:10649976]
GtoPdb - - 7.6 pKi 25.1 nM Ki
ChEMBL Displacement of [125I]RTI55 from DAT B 8.43 pKi 3.7 nM Ki J Med Chem (2008) 51: 2795-2806 [PMID:18393401]
ChEMBL Inhibition of [3H]dopamine reuptake in HEK293 cells expressing human dopamine transporter B 7.74 pIC50 18 nM IC50 J Med Chem (2000) 43: 205-213 [PMID:10649976]
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977]
ChEMBL Binding affinity to dopamine transporter (DAT) using [3H]WIN-35428 as a radioligand B 7.89 pKi 12.88 nM Ki J Med Chem (2000) 43: 4151-4159 [PMID:11063611]
ChEMBL Binding affinity against dopamine transporter labelled with [125I]- RTI-55 in rat. B 8.43 pKi 3.7 nM Ki J Med Chem (1999) 42: 5029-5042 [PMID:10585212]
ChEMBL Binding affinity against Dopamine transporter using [125]RTI-55 B 8.43 pKi 3.7 nM Ki J Med Chem (2001) 44: 3937-3945 [PMID:11689080]
ChEMBL Binding affinity towards dopamine transporter (DAT) B 8.43 pKi 3.7 nM Ki Bioorg Med Chem Lett (2003) 13: 1385-1389 [PMID:12657288]
ChEMBL Binding affinity for dopamine transporter B 8.43 pKi 3.7 nM Ki J Med Chem (2002) 45: 1321-1329 [PMID:11882001]
ChEMBL Reuptake inhibition at the dopamine transporter labeled with radioligand [3H]-5-HT on synaptosomes obtained from whole rat brain minus cerebellum. F 6.53 pIC50 298 nM IC50 J Med Chem (1997) 40: 705-716 [PMID:9057857]
ChEMBL Compound was tested for its ability to inhibit the neurotransmitter dopamine-DA reuptake system using [3H]dopamine as radioligand B 7.43 pIC50 37 nM IC50 Bioorg Med Chem Lett (1997) 7: 2559-2564
ChEMBL Binding against Dopamine transporter using radioligand as [3H]GBR 12935 B 8.39 pIC50 4.1 nM IC50 J Med Chem (1996) 39: 4704-4716 [PMID:8941383]
ChEMBL Binding affinity at the dopamine transporter using [125I]RTI-55 in rat caudate membranes. B 8.43 pIC50 3.7 nM IC50 J Med Chem (1997) 40: 705-716 [PMID:9057857]
ChEMBL Inhibition of dopamine DA reuptake B 8.43 pIC50 3.7 nM IC50 J Med Chem (1996) 39: 4704-4716 [PMID:8941383]
ChEMBL Compound was tested for its ability to inhibit the uptake of [3H]dopamine in DAT (dopamine transporter system) expressing cell line F 8.43 pIC50 3.7 nM IC50 Bioorg Med Chem Lett (1998) 8: 261-266 [PMID:9871666]
ChEMBL Reuptake inhibition at the dopamine transporter labeled with radioligand [3H]dopamine on synaptosomes obtained from rat caudate. F 8.43 pIC50 3.7 nM IC50 J Med Chem (1997) 40: 705-716 [PMID:9057857]
ChEMBL Reuptake inhibition of [3H]-labeled dopamine (DA) in rat. F 8.43 pIC50 3.7 nM IC50 J Med Chem (1999) 42: 5029-5042 [PMID:10585212]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL Binding affinity at the norepinephrine transporter was measured using [125I]RTI-55 as a radioligand B 6.2 pKi 630 nM Ki J Med Chem (2000) 43: 205-213 [PMID:10649976]
ChEMBL Compound was tested for its ability to inhibit the uptake of Norepinephrine in Norepinephrine transporter system F 5.9 pIC50 1261 nM IC50 Bioorg Med Chem Lett (1998) 8: 261-266 [PMID:9871666]
ChEMBL Inhibition of [3H]NE reuptake by human norepinephrine transporter expressed in HEK293 cells B 6.78 pIC50 165 nM IC50 J Med Chem (2000) 43: 205-213 [PMID:10649976]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL Binding affinity for serotonin transporter using [125I]RTI-55 B 5.68 pKi 2090 nM Ki J Med Chem (2000) 43: 205-213 [PMID:10649976]
ChEMBL Displacement of [125I]RTI55 from SERT B 6.21 pKi 620 nM Ki J Med Chem (2008) 51: 2795-2806 [PMID:18393401]
ChEMBL Inhibition of [3H]5-HT reuptake in HEK293 cells expressing human serotonin transporter B 5.43 pIC50 3710 nM IC50 J Med Chem (2000) 43: 205-213 [PMID:10649976]
ChEMBL Compound was tested for its ability to inhibit the uptake of Serotonin in Serotonin transporter system F 6.54 pIC50 289 nM IC50 Bioorg Med Chem Lett (1998) 8: 261-266 [PMID:9871666]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL Binding affinity against Serotonin transporter (SERT) labelled with [125I]RTI-55 in rat. B 6.21 pKi 623 nM Ki J Med Chem (1999) 42: 5029-5042 [PMID:10585212]
ChEMBL Binding affinity towards rat serotonin transporter (SERT) B 6.21 pKi 623 nM Ki Bioorg Med Chem Lett (2003) 13: 1385-1389 [PMID:12657288]
ChEMBL Binding affinity against serotonin transporter using [125]RTI-55 B 6.21 pKi 620 nM Ki J Med Chem (2001) 44: 3937-3945 [PMID:11689080]
ChEMBL Binding affinity for serotonin transporter B 6.21 pKi 620 nM Ki J Med Chem (2002) 45: 1321-1329 [PMID:11882001]
ChEMBL Binding affinity was determined at the Serotonin transporter labeled with radioligand [125 I] RTI-55 B 6.21 pIC50 623 nM IC50 J Med Chem (1997) 40: 705-716 [PMID:9057857]
ChEMBL Reuptake inhibition of [3H]-5-HT (5-HT) in rat. F 6.53 pIC50 298 nM IC50 J Med Chem (1999) 42: 5029-5042 [PMID:10585212]
ChEMBL Compound was tested for its ability to inhibit the neurotransmitter serotonin-5-HT reuptake system using [3H]5-HT as radioligand B 6.54 pIC50 290 nM IC50 Bioorg Med Chem Lett (1997) 7: 2559-2564
ChEMBL Inhibition of [3H]5-HT reuptake at rat serotonin transporter B 6.54 pIC50 289 nM IC50 J Med Chem (1996) 39: 4704-4716 [PMID:8941383]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Sigma receptor binding was determined by labeling with radioligand [3H](+)-pentazocine on frozen membranes obtained from frozen guinea pig brain B 7.77 pIC50 17 nM IC50 J Med Chem (1997) 40: 705-716 [PMID:9057857]
ChEMBL Binding affinity against sigma receptor using radioligand ([3H](+)-pentazocine) binding assay B 7.77 pIC50 17 nM IC50 J Med Chem (1996) 39: 4704-4716 [PMID:8941383]

ChEMBL data shown on this page come from version 32:

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]