EMDT [Ligand Id: 12] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL267615
  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
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  • Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
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  • 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL Compound was evaluated for its binding affinity towards human NET(norepinephrine) transporter B 5 pKi >10000 nM Ki J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 1A receptor B 6.77 pKi 170 nM Ki J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
GtoPdb - - 6.8 pKi - - - J Med Chem (2000) 43: 1011-8 [PMID:10715164]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 1A receptor in rat B 6 pIC50 >1000 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 1B receptor in rat B 6 pIC50 >1000 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 6.5 pKi - - - J Med Chem (2000) 43: 1011-8 [PMID:10715164]
ChEMBL Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 1D receptor B 6.54 pKi 290 nM Ki J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 1D receptor in calf B 5.85 pIC50 1400 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
ChEMBL Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 1E receptor B 6.28 pKi 520 nM Ki J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
GtoPdb - - 6.3 pKi - - - J Med Chem (2000) 43: 1011-8 [PMID:10715164]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 2A receptor in human B 6.21 pIC50 620 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Compound was evaluated for its binding affinity towards rat 5-hydroxytryptamine 2A receptor B 5 pKi >10000 nM Ki J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 2C receptor in human B 5.26 pIC50 5500 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
ChEMBL Compound was evaluated for its binding affinity towards rat 5-hydroxytryptamine 2C receptor B 5.74 pKi 1810 nM Ki J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 3 receptor expressed in NG 108 cells B 6 pIC50 >1000 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig B 7.36 pIC50 44 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
GtoPdb - - 5.3 pKi - - - J Med Chem (2000) 43: 1011-8 [PMID:10715164]
ChEMBL Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor B 5.34 pKi 4620 nM Ki J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand B 7.28 pKi 52 nM Ki J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
ChEMBL Binding affinity for human 5-hydroxytryptamine 6 receptor B 7.3 pKi <50 nM Ki J Med Chem (2005) 48: 1781-1795 [PMID:15771424]
ChEMBL Binding affinity against 5 Hydroxy tryptamine 6 receptor B 7.8 pKi 16 nM Ki Bioorg Med Chem Lett (2005) 15: 1707-1711 [PMID:15745826]
ChEMBL Binding affinity against 5-hydroxytryptamine 6 receptor B 7.8 pKi 16 nM Ki Bioorg Med Chem Lett (2004) 14: 4569-4573 [PMID:15357994]
ChEMBL Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells B 7.8 pKi 16 nM Ki J Med Chem (2008) 51: 603-611 [PMID:18201064]
ChEMBL Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting B 7.8 pKi 16 nM Ki J Med Chem (2009) 52: 675-687 [PMID:19159187]
ChEMBL Binding affinity to 5HT6 receptor B 7.8 pKi 16 nM Ki Bioorg Med Chem (2009) 17: 7387-7397 [PMID:19758807]
ChEMBL Binding affinity to 5-HT6 receptor (unknown origin) B 7.8 pKi 16 nM Ki Med Chem Res (2005) 14: 1-18
ChEMBL Binding affinity towards human 5-hydroxytryptamine 6 receptor B 7.8 pKi 16 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometry B 7.8 pKi 16 nM Ki J Med Chem (2015) 58: 7901-7912 [PMID:26099069]
ChEMBL Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor B 7.8 pKi 16 nM Ki J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
GtoPdb - - 7.8 pKi - - - J Med Chem (2000) 43: 1011-8 [PMID:10715164]
ChEMBL Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor stably expressed in HEK cells B 7.07 pIC50 85 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 6 receptor in human B 7.07 pIC50 85 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
GtoPdb - - 6.5 pKi - - - J Med Chem (2000) 43: 1011-8 [PMID:10715164]
ChEMBL Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 7 receptor B 6.52 pKi 300 nM Ki J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 7 receptor in human B 5.82 pIC50 1500 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL Compound was evaluated for its binding affinity towards human serotonin transporter B 5 pKi >10000 nM Ki J Med Chem (2000) 43: 1011-1018 [PMID:10715164]

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]