5-MeOT [Ligand Id: 107] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL8165
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  • Norepinephrine transporter in Rat [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
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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 Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
  • 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-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor in Rat [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-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
  • 5-HT4 receptor in Mouse [GtoPdb: 9] [UniProtKB: P97288]
  • 5-HT4 receptor in Rat [GtoPdb: 9] [UniProtKB: Q62758]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
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  • TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7]
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  • 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
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  • 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
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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 Induction of DAT-mediated dopamine release in rat brain synaptosomes by [3H]DA release assay B 4.96 pEC50 11031 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 4754-4758 [PMID:25193229]
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
ChEMBL Induction of NET-mediated norepinephrine release in rat brain synaptosomes by [3H]NE release assay B 5 pEC50 >10000 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 4754-4758 [PMID:25193229]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL In vitro affinity at human cloned 5-hydroxytryptamine 1A receptor by [3H]8-OH-DPAT displacement. B 8.49 pKi 3.2 nM Ki J. Med. Chem. (1996) 39: 314-322 [PMID:8568822]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement B 7.97 pKi 10.72 nM Ki J. Med. Chem. (1996) 39: 126-134 [PMID:8568799]
ChEMBL Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand. B 8.05 pKi 9 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
ChEMBL Binding affinity against 5-hydroxytryptamine 1A receptor using [3H]-8-OH-DPAT as radioligand B 8.3 pKi 5 nM Ki J. Med. Chem. (1990) 33: 2777-2784 [PMID:2213830]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor B 8.49 pKi 3.2 nM Ki J. Med. Chem. (1988) 31: 867-870 [PMID:2965244]
ChEMBL Binding affinity of compound towards 5-hydroxytryptamine 1A receptor in rat striatal membranes by [3H]OH-DPAT displacement. B 8.49 pKi 3.2 nM Ki J. Med. Chem. (1989) 32: 1921-1926 [PMID:2754715]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 7.5 pKi - - - Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658];
J Neurochem (1996) 67: 2096-103 [PMID:8863519]
ChEMBL Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta B 8.46 pKi 3.5 nM Ki J. Med. Chem. (1996) 39: 314-322 [PMID:8568822]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand. B 6.4 pKi 400 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
ChEMBL Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand. B 6.4 pKi 400 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
ChEMBL Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate B 8.19 pKi 6.46 nM Ki J. Med. Chem. (1988) 31: 1406-1412 [PMID:3385733]
ChEMBL Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptor B 8.4 pKi 4 nM Ki J. Med. Chem. (1988) 31: 867-870 [PMID:2965244]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL Selectivity towards 5-hydroxytryptamine 1D receptor beta to that of 5-hydroxytryptamine 1D receptor alpha B 8.27 pKi 5.4 nM Ki J. Med. Chem. (1996) 39: 314-322 [PMID:8568822]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1D receptor was determined in calf striatum homogenate B 8.39 pKi 4.1 nM Ki J. Med. Chem. (1996) 39: 314-322 [PMID:8568822]
GtoPdb - - 8.7 pKi - - - Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658];
Mol Pharmacol (1996) 50: 1567-80 [PMID:8967979];
Mol Pharmacol (1991) 40: 143-8 [PMID:1652050]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Affinity against 5-hydroxytryptamine 2A receptor (K) labeled with [3H]ketanserin. B 6.52 pKi 300 nM Ki J. Med. Chem. (1994) 37: 1929-1935 [PMID:8027974]
ChEMBL Affinity against 5-hydroxytryptamine 2A receptor (D) labeled with [125I]DOI. B 8.32 pKi 4.8 nM Ki J. Med. Chem. (1994) 37: 1929-1935 [PMID:8027974]
GtoPdb - - 8.9 pKi - - - Mol Pharmacol (1994) 45: 277-86 [PMID:8114677]
ChEMBL Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay F 9.3 pEC50 0.5 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 4754-4758 [PMID:25193229]
5-HT2A receptor in Rat [GtoPdb: 6] [UniProtKB: P14842]
GtoPdb - - 8.1 pKi - - - Mol Pharmacol (1994) 45: 277-86 [PMID:8114677]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Evaluated for the binding affinity to porcine choroid plexus at 5-hydroxytryptamine 2C receptor binding site by using [3H]-MES as a radioligand. B 7.35 pKi 45 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
GtoPdb - - 7.8 pKi - - - Synapse (2000) 35: 144-150 [PMID:10611640]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
GtoPdb - - 6.3 pKi - - - J Neurochem (1997) 69: 1138-44 [PMID:9282936]
ChEMBL Affinity against 5-hydroxytryptamine 2C receptor in J1 cells transfected with the rat 5-HT2C gene labeled with [3H]mesulergine. B 6.3 pKi 500 nM Ki J. Med. Chem. (1994) 37: 1929-1935 [PMID:8027974]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
ChEMBL Displacement of [3H]GR-113808 from human recombinant 5HT4b receptor expressed in HEK293 cells by scintillation counting B 6.61 pKi 245.47 nM Ki Eur. J. Med. Chem. (2009) 44: 2952-2959 [PMID:19223092]
GtoPdb - - 6.8 pKi - - - J Neurochem (1997) 69: 1810-9 [PMID:9349523];
J Neurochem (1998) 70: 2252-61 [PMID:9603189];
J Neurochem (2000) 74: 478-89 [PMID:10646498];
Naunyn Schmiedebergs Arch Pharmacol (2001) 363: 146-60 [PMID:11218067];
Br J Pharmacol (2000) 129: 771-81 [PMID:10683202];
Br J Pharmacol (2000) 131: 827-35 [PMID:11030734]
ChEMBL Displacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation counting B 7.57 pKi 26.92 nM Ki Eur. J. Med. Chem. (2009) 44: 2952-2959 [PMID:19223092]
5-HT4 receptor in Mouse [GtoPdb: 9] [UniProtKB: P97288]
GtoPdb - - 6.6 pKi - - - FEBS Lett (1996) 398: 19-25 [PMID:8946946]
5-HT4 receptor in Rat [GtoPdb: 9] [UniProtKB: Q62758]
GtoPdb - - 7.4 pKi - - - EMBO J (1995) 14: 2806-15 [PMID:7796807];
Eur J Pharmacol (1996) 304: 231-5 [PMID:8813606];
Neuropharmacology (1997) 36: 671-9 [PMID:9225293]
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 7.06 pKi 88 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]
GtoPdb - - 7.4 pKi - - - J Neurochem (1996) 66: 47-56 [PMID:8522988]
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 8.4 pKi - - - Mol Pharmacol (1993) 43: 320-7 [PMID:7680751];
Neuropharmacology (1997) 36: 713-20 [PMID:9225298];
J Neurochem (1998) 71: 2169-77 [PMID:9798944]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells B 8.3 pKi 5.01 nM Ki Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003]
ChEMBL Binding affinity of compound towards rodent 5-hydroxytryptamine 7 receptor B 8.7 pKi 2 nM Ki J. Med. Chem. (2003) 46: 2795-2812 [PMID:12825922]
GtoPdb - - 9.5 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2001) 363: 620-32 [PMID:11414657];
Br J Pharmacol (1997) 122: 126-32 [PMID:9298538];
J Biol Chem (1993) 268: 23422-6 [PMID:8226867]
5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
GtoPdb - - 8.2 pKi - - - Mol Pharmacol (1993) 44: 229-36 [PMID:8394987]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
ChEMBL Binding affinity at rat 5-hydroxytryptamine 7 receptor. B 9.03 pKi 0.93 nM Ki J. Med. Chem. (2003) 46: 5365-5374 [PMID:14640545]
GtoPdb - - 9.2 pKi - - - J Biol Chem (1993) 268: 18200-4 [PMID:8394362];
Proc Natl Acad Sci USA (1993) 90: 8547-51 [PMID:8397408]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL Induction of 5-HTT-mediated 5-HT release in rat brain synaptosomes by [3H]5-HT release assay B 5.66 pEC50 2169 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 4754-4758 [PMID:25193229]
TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7]
ChEMBL Antagonist activity at human TRPM8 receptor expressed in human T-REx-293 cells assessed as inhibition of menthol-induced 45calcium influx treated 5 mins before menthol challenge measured after 5 mins F 4.91 pIC50 12400 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 7076-7079 [PMID:20965726]
ChEMBL Antagonist activity at human TRPM8 receptor expressed in human T-REx-293 cells assessed as inhibition of icilin-induced 45calcium influx treated 5 mins before icilin challenge measured after 5 mins F 4.94 pIC50 11600 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 7076-7079 [PMID:20965726]
5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
GtoPdb - - 6.2 pKi - - - J Neurochem (1996) 67: 2096-103 [PMID:8863519];
Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639];
Eur J Pharmacol (2004) 484: 127-39 [PMID:14744596];
Bioorg Med Chem (2004) 12: 2545-52 [PMID:15110837]
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
GtoPdb - - 5.9 pKi - - - Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]
5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
GtoPdb - - 8 pKi - - - Mol Pharmacol (1993) 43: 419-26 [PMID:8450835]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]