ChEMBL ligand: CHEMBL1508 (Cipralex, Escitalopram, Esertia, Esitol, LU-26-054)
DAT/Dopamine transporter in Rat [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] 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!
Transporter in Rat [ChEMBL: CHEMBL6184] [UniProtKB: Q63380] 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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977]
ChEMBL	Displacement of [3H]WIN-35428 from DAT in rat caudate-putamen by scintillation counting	B	5.09	pKi	8150	nM	Ki	J Med Chem (2010) 53: 6112-6121 [PMID:20672825]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL	Binding affinity to human SERT expressed in African green monkey COS7 cells after 2 hrs by scintillation counting analysis	B	8.59	pKd	2.6	nM	Kd	ACS Med Chem Lett (2014) 5: 696-699 [PMID:24944746]
GtoPdb	-	-	8.68	pKd	2.1	nM	Kd	Nature (2016) 532: 334-9 [PMID:27049939]
ChEMBL	Inhibition of human SERT S438T mutant expressed in HEK293 GripTite cells pre-incubated for 5 mins followed by [3H]5-HT addition by [3H]5-HT uptake assay	B	5.1	pKi	7879	nM	Ki	J Med Chem (2015) 58: 5609-5619 [PMID:26153715]
ChEMBL	Inhibition of 5-hydroxy[3H]tryptamine uptake at human SERT expressed in African green monkey COS7 cells incubated for 10 mins prior to radioligand addition measured after 5 mins by scintillation counting analysis	B	8.13	pKi	7.4	nM	Ki	ACS Med Chem Lett (2014) 5: 696-699 [PMID:24944746]
ChEMBL	Inhibition of wild type human SERT expressed in HEK293 GripTite cells pre-incubated for 5 mins followed by [3H]5-HT addition by [3H]5-HT uptake assay	B	8.66	pKi	2.2	nM	Ki	J Med Chem (2015) 58: 5609-5619 [PMID:26153715]
ChEMBL	Displacement of [125I]-RTI-55 from human SERT expressed in HEK293 cell membranes after 1 hr by gamma counting method	B	8.75	pKi	1.77	nM	Ki	Bioorg Med Chem Lett (2018) 28: 3431-3435 [PMID:30266542]
ChEMBL	Displacement of [3H]citalopram from human serotonin transporter expressed in HEK293 cells by scintillation proximity assay	B	9	pKi	1	nM	Ki	Bioorg Med Chem Lett (2009) 19: 5552-5555 [PMID:19720528]
ChEMBL	Displacement of [3H]citalopram form human SRET by liquid scintillation counting	B	9	pKi	1	nM	Ki	Bioorg Med Chem Lett (2010) 20: 2983-2986 [PMID:20347298]
ChEMBL	Allosteric modulation at wild-type human SERT site S2 expressed in african green monkey COS7 cells assessed as inhibition of [3H]citalopram dissociation at 30 uM by scintillation counting analysis	B	5.34	pIC50	4600	nM	IC50	J Med Chem (2013) 56: 9709-9724 [PMID:24237160]
ChEMBL	Displacement of [3H]-S-citalopram from human SERT primary site (S1) expressed in African green monkey COS7 cell membranes after 2 hrs by microbeta scintillation counting method	B	8	pIC50	10	nM	IC50	Bioorg Med Chem Lett (2017) 27: 470-478 [PMID:28041833]
ChEMBL	Inhibition of [3H]5-HT uptake by SERT primary site (S1) (unknown origin) expressed in African green monkey COS1 cells after 10 mins by TopCount scintillation counting method	B	8.68	pIC50	2.1	nM	IC50	Bioorg Med Chem Lett (2017) 27: 470-478 [PMID:28041833]
GtoPdb	-	-	9	pIC50	1	nM	IC50	Bioorg Med Chem Lett (2009) 19: 5552-5 [PMID:19720528]
ChEMBL	Inhibition of [3H]-S-citalopram dissociation from human SERT allosteric modulator site (S2) expressed in African green monkey COS7 cell membranes after 80 mins by microbeta scintillation counting method	B	5.24	pEC50	5800	nM	EC50	Bioorg Med Chem Lett (2017) 27: 470-478 [PMID:28041833]
ChEMBL	Inhibition of [3H]-S-citalopram dissociation from SERT allosteric modulator site (S2) (unknown origin) expressed in African green monkey COS1 cell membranes by scintillation counting method	B	5.29	pEC50	5100	nM	EC50	Bioorg Med Chem Lett (2017) 27: 470-478 [PMID:28041833]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL	Displacement of [3H]citalopram from SERT in rat brain stem by scintillation counting	B	9.05	pKi	0.89	nM	Ki	J Med Chem (2010) 53: 6112-6121 [PMID:20672825]
Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380]
ChEMBL	Displacement of [3H]nisoxetine from NET in rat frontal cortex by scintillation counting	B	4.98	pKi	10500	nM	Ki	J Med Chem (2010) 53: 6112-6121 [PMID:20672825]

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]