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: 144-150 [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 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
