tryptamine [Ligand Id: 125] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL6640 |
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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: 144-50 [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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5857] [GtoPdb: 364] [UniProtKB: Q96RJ0] | ||||||||
| ChEMBL | Agonist activity at recombinant human TAAR1 expressed in CHO-K1 cells assessed as increase in intracellular cAMP incubated for 30 mins by HTRF analysis | F | 5.66 | pEC50 | 2210 | nM | EC50 | ACS Med Chem Lett (2022) 13: 92-98 [PMID:35047111] |
| 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 | F | 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 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]
