5-CT [Ligand Id: 4] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL18840 (5-Carboxamidotryptamine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Binding affinity to 5HT1A receptor | B | 9.4 | pKd | 0.4 | nM | Kd | J Med Chem (2009) 52: 6107-6125 [PMID:19754201] |
| ChEMBL | Binding affinity for 5-hydroxytryptamine 1A receptor was determined | B | 9.5 | pKd | 9.5 | - | pKD | J Med Chem (1993) 36: 1918-1919 [PMID:8515429] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1A human cloned receptors in HEK293 cells using [3H]8-OH-DPAT as radioligand | B | 9.2 | pKi | 0.63 | nM | Ki | J Med Chem (2003) 46: 5117-5120 [PMID:14613313] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cell membranes measured after 120 mins | B | 9.47 | pKi | 0.34 | nM | Ki | Eur J Med Chem (2019) 180: 673-689 [PMID:31357129] |
| ChEMBL | Binding affinity was measured on cloned Human 5-hydroxytryptamine 1A receptor which is labeled by [3H]8-OH-DPAT | B | 9.52 | pKi | <0.3 | nM | Ki | J Med Chem (2000) 43: 1339-1349 [PMID:10753471] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells membrane incubated for 1 hr by microbeta liquid scintillation counting analysis | B | 9.59 | pKi | 0.26 | nM | Ki | Eur J Med Chem (2023) 252: 115285-115285 [PMID:37027998] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK cell membrane incubated for 120 mins by microplate beta scintillation counting analysis | B | 9.7 | pKi | 0.2 | nM | Ki | Bioorg Med Chem (2023) 84: 117256-117256 [PMID:37003157] |
| GtoPdb | - | - | 10.3 | pKi | - | - | - |
Biochem J (1992) 285 ( Pt 3): 933-8 [PMID:1386736]; Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 205-17 [PMID:9550290]; Naunyn Schmiedebergs Arch Pharmacol (1997) 355: 682-8 [PMID:9205951] |
| ChEMBL | In Vitro Binding affinity againist 5-HT1A receptor by displacing [3H]8-OH-DPAT from pig cortex | B | 9.53 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 1207-1212 |
| ChEMBL | Agonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 mins | F | 9.57 | pEC50 | 0.27 | nM | EC50 | Eur J Med Chem (2023) 252: 115285-115285 [PMID:37027998] |
| ChEMBL | Agonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 mins | F | 9.57 | pEC50 | 0.27 | nM | EC50 | Eur J Med Chem (2023) 252: 115285-115285 [PMID:37027998] |
| 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 | 9.53 | pKi | 0.3 | 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 | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| GtoPdb | - | - | 8.8 | pKi | - | - | - |
Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658]; J Neurochem (1996) 67: 2096-103 [PMID:8863519] |
| ChEMBL | Binding affinity against human 5-hydroxytryptamine 1B receptor cloned receptors in CHO cells | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (2003) 46: 5117-5120 [PMID:14613313] |
| 5-HT1B receptor in Mouse [GtoPdb: 2] [UniProtKB: P28334] | ||||||||
| GtoPdb | - | - | 8.1 | pKi | - | - | - | Proc Natl Acad Sci USA (1992) 89: 3020-4 [PMID:1557407] |
| 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 | 8.3 | pKi | 5 | 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 | Binding affinity for 5-hydroxytryptamine 1D receptor was determined | B | 8.8 | pKd | 8.8 | - | pKD | J Med Chem (1993) 36: 1918-1919 [PMID:8515429] |
| GtoPdb | - | - | 9.2 | 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] |
| ChEMBL | In Vitro Binding affinity againist 5-hydroxytryptamine 1D receptor by displacing [125I]GTI from pig caudate | B | 8.47 | pIC50 | 3.39 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 1207-1212 |
| Serotonin 1d (5-HT1d) receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105] [UniProtKB: P79400] | ||||||||
| ChEMBL | Binding activity against 5-hydroxytryptamine 1D receptor from pig caudate membrane using [3H]5-HT as radioligand | B | 8.4 | pIC50 | 3.98 | nM | IC50 | J Med Chem (1995) 38: 1799-1810 [PMID:7752204] |
| ChEMBL | Displacement of radioligand [3H]5-HT binding to 5-hydroxytryptamine 1D receptor in pig caudate membrane | B | 8.4 | pIC50 | 3.98 | nM | IC50 | J Med Chem (1993) 36: 1529-1538 [PMID:8496922] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 2A receptor human cloned receptors in HEK 293 cells using [3H]ketanserin as radioligand | B | 5.3 | pKi | <5011.87 | nM | Ki | J Med Chem (2003) 46: 5117-5120 [PMID:14613313] |
| GtoPdb | - | - | 6.5 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| ChEMBL | In Vitro Binding affinity againist 5-HT2A receptor by displacing [3H]-DOB from rat cortex homogenates | B | 4.66 | pIC50 | 21877.62 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 1207-1212 |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 2C receptor human cloned receptors in HEK 293 cells using [3H]mesulergine as radioligand | B | 5.6 | pKi | 2511.89 | nM | Ki | J Med Chem (2003) 46: 5117-5120 [PMID:14613313] |
| 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 | 6.21 | pKi | 620 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| GtoPdb | - | - | 6.7 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Synapse (2000) 35: 144-50 [PMID:10611640] |
| ChEMBL | In Vitro Binding affinity againist 5-hydroxytryptamine 2C receptor by displacing [3H]mesulergine from pig cortex | B | 6.23 | pIC50 | 588.84 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 1207-1212 |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
| ChEMBL | Binding affinity for 5-hydroxytryptamine 1C receptor was determined | B | 6.2 | pKd | 6.2 | - | pKD | J Med Chem (1993) 36: 1918-1919 [PMID:8515429] |
| 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 5A receptor | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| GtoPdb | - | - | 7.7 | pKi | - | - | - |
FEBS Lett (1994) 355: 242-6 [PMID:7988681]; Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685] |
| 5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966] | ||||||||
| GtoPdb | - | - | 7.8 | pKi | - | - | - |
Mol Pharmacol (1993) 43: 313-9 [PMID:8450829]; Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685]; FEBS Lett (1995) 377: 451-6 [PMID:8549774] |
| 5-HT5A receptor in Rat [GtoPdb: 10] [UniProtKB: P35364] | ||||||||
| GtoPdb | - | - | 7.9 | pKi | - | - | - | Proc Natl Acad Sci USA (1993) 90: 3452-6 [PMID:7682702] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand | B | 6 | pKi | 1000 | nM | Ki | J Med Chem (2003) 46: 5117-5120 [PMID:14613313] |
| GtoPdb | - | - | 6.1 | pKi | - | - | - | J Neurochem (1996) 66: 47-56 [PMID:8522988] |
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand | B | 6.14 | pKi | 720 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388] | ||||||||
| GtoPdb | - | - | 6.7 | 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 | Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileum | B | 7.48 | pKd | 33.11 | nM | Kd | J Med Chem (2004) 47: 6616-6624 [PMID:15588097] |
| ChEMBL | Binding affinity of compound towards rodent 5-hydroxytryptamine 7 receptor | B | 8 | pKi | <10 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Binding affinity to 5-HT7 receptor (unknown origin) | B | 9.03 | pKi | 0.93 | nM | Ki | J Med Chem (2018) 61: 8475-8503 [PMID:29767995] |
| ChEMBL | Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Binding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligand | B | 9.31 | pKi | 0.49 | nM | Ki | J Med Chem (2002) 45: 2197-2206 [PMID:12014957] |
| ChEMBL | Displacement of [3H]-5-CT from human recombinant 5-HT7 receptor expressed in CHO-K1 cells after 120 mins | B | 9.4 | pKi | 0.4 | nM | Ki | Eur J Med Chem (2013) 69: 920-930 [PMID:24161678] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 7 human receptors | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2003) 46: 5117-5120 [PMID:14613313] |
| ChEMBL | Displacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 60 mins by radioligand binding assay | B | 9.46 | pKi | 0.35 | nM | Ki | Eur J Med Chem (2020) 199: 112395-112395 [PMID:32442850] |
| GtoPdb | - | - | 10 | 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]; Br J Pharmacol (1998) 124: 1300-6 [PMID:9720804] |
| ChEMBL | Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum | F | 6.2 | pEC50 | 630 | nM | EC50 | J Med Chem (2004) 47: 6616-6624 [PMID:15588097] |
| ChEMBL | Agonist activity at human 5HT7 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay | F | 8.29 | pEC50 | 5.1 | nM | EC50 | Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805] |
| 5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304] | ||||||||
| GtoPdb | - | - | 9 | 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 | Displacement of [3H]-5-CT from 5-HT7 receptor in Sprague-Dawley rat hypothalamus after 120 mins | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (2013) 56: 7851-7861 [PMID:24050112] |
| ChEMBL | Binding affinity to the rat 5-hydroxytryptamine 7 receptor | B | 9.29 | pKi | 0.51 | nM | Ki | J Med Chem (2003) 46: 646-649 [PMID:12570387] |
| ChEMBL | Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells | B | 9.29 | pKi | 0.51 | nM | Ki | J Med Chem (2004) 47: 6616-6624 [PMID:15588097] |
| ChEMBL | Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells | B | 9.29 | pKi | 0.51 | nM | Ki | Bioorg Med Chem (2007) 15: 5316-5321 [PMID:17517509] |
| ChEMBL | Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2007) 50: 4214-4221 [PMID:17649988] |
| ChEMBL | Displacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cells | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2008) 51: 5813-5822 [PMID:18800769] |
| GtoPdb | - | - | 9.9 | pKi | - | - | - |
J Biol Chem (1993) 268: 18200-4 [PMID:8394362]; Proc Natl Acad Sci USA (1993) 90: 8547-51 [PMID:8397408] |
| ChEMBL | Binding affinity at rat 5-hydroxytryptamine 7 receptor. | B | 9.92 | pKi | 0.12 | nM | Ki | J Med Chem (2003) 46: 5365-5374 [PMID:14640545] |
| ChEMBL | Binding affinity against Rat 5-hydroxytryptamine 7 receptor using [3H]5-HT | B | 10.54 | pKi | 0.03 | nM | Ki | J Med Chem (2000) 43: 1339-1349 [PMID:10753471] |
| Serotonin 7 (5-HT7) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5494] [UniProtKB: P50407] | ||||||||
| ChEMBL | Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction | F | 6.2 | pEC50 | 630 | nM | EC50 | J Med Chem (2007) 50: 4214-4221 [PMID:17649988] |
| ChEMBL | Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction | F | 6.2 | pEC50 | 630 | nM | EC50 | J Med Chem (2008) 51: 5813-5822 [PMID:18800769] |
| 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| GtoPdb | - | - | 5.5 | pKi | - | - | - |
J Neurochem (1996) 67: 2096-103 [PMID:8863519]; Proc Natl Acad Sci USA (1992) 89: 5517-21 [PMID:1608964]; Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]; Eur J Pharmacol (2004) 484: 127-39 [PMID:14744596] |
| 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939] | ||||||||
| GtoPdb | - | - | 6.1 | pKi | - | - | - |
Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]; Neuropharmacology (1997) 36: 569-76 [PMID:9225282] |
| 5-HT1F receptor in Rat [GtoPdb: 5] [UniProtKB: P30940] | ||||||||
| GtoPdb | - | - | 5.6 | pIC50 | - | - | - | Proc Natl Acad Sci USA (1993) 90: 2184-8 [PMID:8384716] |
| 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| GtoPdb | - | - | 6.9 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Mol Pharmacol (1994) 46: 227-34 [PMID:8078486] |
| 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994] | ||||||||
| GtoPdb | - | - | 6.8 | pKi | - | - | - |
Mol Pharmacol (1994) 46: 227-34 [PMID:8078486]; Mol Pharmacol (1993) 43: 419-26 [PMID:8450835] |
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]
