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ChEMBL ligand: CHEMBL26320 (GBR-12935) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]