ChEMBL ligand: CHEMBL26320 (GBR-12935)
DAT/Dopamine transporter in Human [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] DAT/Dopamine transporter in Rat [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] There should be some charts here, you may need to enable JavaScript!
NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] There should be some charts here, you may need to enable JavaScript!
SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] SERT/Serotonin transporter in Rat [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] There should be some charts here, you may need to enable JavaScript!
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] There should be some charts here, you may need to enable JavaScript!

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 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]