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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]