tryptamine [Ligand Id: 125] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL6640
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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 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-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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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 Rat [GtoPdb: 12] [UniProtKB: P32305]
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  • TA1 receptor/Trace amine-associated receptor 1 in Rat [ChEMBL: CHEMBL3833] [GtoPdb: 364] [UniProtKB: Q923Y9]
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cathepsin K/Cathepsin K in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL268] [GtoPdb: 2350] [UniProtKB: P43235]
ChEMBL Inhibition of cathepsin K by fluorimetric assay B 4.82 pIC50 15000 nM IC50 J. Nat. Prod. (2002) 65: 628-629 [PMID:11975521]
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 6.79 pEC50 164 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 4754-4758 [PMID:25193229]
myeloperoxidase/Myeloperoxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2439] [GtoPdb: 2789] [UniProtKB: P05164]
ChEMBL Inhibition of human recombinant MPO-mediated taurine chlorination after 5 mins by microplate assay B 6.11 pIC50 770 nM IC50 J. Med. Chem. (2013) 56: 3943-3958 [PMID:23581551]
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 6.15 pEC50 716 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 4754-4758 [PMID:25193229]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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 6.77 pKi 170 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
ChEMBL Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement B 6.77 pKi 169.82 nM Ki J. Med. Chem. (1996) 39: 126-134 [PMID:8568799]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 6.3 pKi - - - Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658]
ChEMBL Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta B 7.44 pKi 36 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 4.99 pKi 10200 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL In vitro affinity human cloned 5-hydroxytryptamine 1D receptor alpha by [3H]5-HT displacement. B 7.21 pKi 61 nM Ki J. Med. Chem. (1996) 39: 314-322 [PMID:8568822]
GtoPdb - - 7.4 pKi - - - Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658];
Mol Pharmacol (1996) 50: 1567-80 [PMID:8967979]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1D receptor was determined in calf striatum homogenate B 7.64 pKi 23 nM Ki J. Med. Chem. (1996) 39: 314-322 [PMID:8568822]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 7.6 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733];
Mol Pharmacol (1990) 38: 604-9 [PMID:2233697];
Mol Pharmacol (1994) 45: 277-86 [PMID:8114677]
ChEMBL Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay F 8.13 pEC50 7.36 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 4754-4758 [PMID:25193229]
5-HT2A receptor in Rat [GtoPdb: 6] [UniProtKB: P14842]
GtoPdb - - 7.1 pKi - - - Mol Pharmacol (1994) 45: 277-86 [PMID:8114677]
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb - - 7 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994]
ChEMBL The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus B 6.27 pKd 537.03 nM Kd J. Med. Chem. (1982) 25: 68-70 [PMID:7086824]
GtoPdb - - 7 pKi - - - Mol Pharmacol (1993) 43: 419-26 [PMID:8450835]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
GtoPdb - - 7.2 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733];
Synapse (2000) 35: 144-150 [PMID:10611640]
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 7.3 pKi 50 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
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 6.74 pKi 180 nM Ki J. Med. Chem. (2000) 43: 1011-1018 [PMID:10715164]
ChEMBL Binding affinity to Homo sapiens (human) 5-HT6 receptor B 7.15 pKi 70 nM Ki Med Chem Res (2005) 14: 1-18
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 6.8 pKi - - - Mol Pharmacol (1993) 43: 320-7 [PMID:7680751];
Neuropharmacology (1997) 36: 713-20 [PMID:9225298]
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 6.8 pKi 158.49 nM Ki Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003]
GtoPdb - - 6.8 pKi - - - J Biol Chem (1993) 268: 23422-6 [PMID:8226867]
5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
GtoPdb - - 7.8 pKi - - - J Biol Chem (1993) 268: 18200-4 [PMID:8394362]
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 7.49 pEC50 32.6 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 4754-4758 [PMID:25193229]
TA1 receptor/Trace amine-associated receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3833] [GtoPdb: 364] [UniProtKB: Q923Y9]
ChEMBL Agonist activity at rat N-terminal FLAG-tagged TAAR1 expressed in HEK293 cells assessed as [3H]cAMP accumulation measured after 1 hr B 6.51 pEC50 310 nM EC50 J Med Chem (2017) 60: 2605-2628 [PMID:28244748]
5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
GtoPdb - - 6.5 pKi - - - 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 - - 5.6 pKi - - - Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]

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]