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] |
| 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 |
| 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: 144-150 [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 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]
