5-hydroxytryptamine [Ligand Id: 5] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL39 (5-HT, 5-Hydroxytryptamine, Enteramine, Serotonin, Thrombotonin)
  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • MT1 receptor/Melatonin receptor 1A in Human [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039]
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  • MT2 receptor/Melatonin receptor 1B in Human [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264]
  • 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 in Mouse [GtoPdb: 2] [UniProtKB: P28334]
  • 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]
  • Serotonin 1d (5-HT1d) receptor in Pig [ChEMBL: CHEMBL4105] [UniProtKB: P79400]
  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Rat [ChEMBL: CHEMBL5450] [GtoPdb: 3] [UniProtKB: P28565]
  • Serotonin 1d (5-HT1d) receptor in Guinea pig [ChEMBL: CHEMBL2304407] [UniProtKB: Q60484]
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  • 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939]
  • 5-HT1F receptor in Rat [GtoPdb: 5] [UniProtKB: P30940]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Mouse [ChEMBL: CHEMBL5377] [GtoPdb: 6] [UniProtKB: P35363]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [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]
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Mouse [ChEMBL: CHEMBL4972] [GtoPdb: 373] [UniProtKB: P23979]
  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Rat [ChEMBL: CHEMBL2411] [GtoPdb: 373] [UniProtKB: P35563]
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  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
  • 5-HT4 receptor in Mouse [GtoPdb: 9] [UniProtKB: P97288]
  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
  • Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
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  • 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
  • 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Mouse [ChEMBL: CHEMBL3597] [GtoPdb: 10] [UniProtKB: P30966]
  • 5-HT5A receptor in Rat [GtoPdb: 10] [UniProtKB: P35364]
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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 Mouse [GtoPdb: 12] [UniProtKB: P32304]
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
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  • Organic cation transporter 3/Solute carrier family 22 member 3 in Rat [ChEMBL: CHEMBL1770033] [GtoPdb: 1021] [UniProtKB: O88446]
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  • Vesicular monoamine transporter 2/Synaptic vesicular amine transporter in Human [ChEMBL: CHEMBL1893] [GtoPdb: 1012] [UniProtKB: Q05940]
  • Vesicular monoamine transporter 2/Synaptic vesicular amine transporter in Mouse [ChEMBL: CHEMBL4295886] [GtoPdb: 1012] [UniProtKB: Q8BRU6]
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  • D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
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  • 5-HT3AB in Human [GtoPdb: 378]
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  • 5-HT3A in Human [GtoPdb: 379]
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  • Proton-coupled Amino acid Transporter 1 in Human [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells B 5.01 pKd 9690 nM Kd J. Med. Chem. (1996) 39: 850-859 [PMID:8632409]
GtoPdb - - 5 pKi - - - Nature (1991) 350: 614-9 [PMID:1826762]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Basal binding towards Dopamine receptor D3 was evaluated using [35S]- GTP-gamma S radioligand B 6.28 pEC50 523 nM EC50 J. Med. Chem. (2003) 46: 3822-3839 [PMID:12930145]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. B 5.63 pKi 2338 nM Ki J. Med. Chem. (1993) 36: 1499-1500 [PMID:8098771]
MT1 receptor/Melatonin receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039]
ChEMBL Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells B 4 pKi >100000 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 2409-2414
MT2 receptor/Melatonin receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286]
ChEMBL Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1B expressed in CHO cells B 4 pKi >100000 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 2409-2414
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity for 5-hydroxytryptamine 1A receptor was determined B 8.5 pKd 8.5 - pKD J. Med. Chem. (1993) 36: 1918-1919 [PMID:8515429]
ChEMBL Displacement of [3H]WAY100635 from human recombinant 5HT1A receptor B 5 pKi 10000 nM Ki J. Med. Chem. (2008) 51: 2887-2890 [PMID:18433113]
ChEMBL Displacement of [3H]8-OH-DPAT from 5HT1A receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting B 7.3 pKi <50 nM Ki Bioorg. Med. Chem. (2010) 18: 3345-3351 [PMID:20363635]
ChEMBL Displacement of [3H]-8-OH-DPAT from human recombinant 5-HT1A receptor expressed in HEK293-EBNA cells after 120 mins B 8.02 pKi 9.5 nM Ki Eur. J. Med. Chem. (2013) 69: 920-930 [PMID:24161678]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in CHO-K1 cell membranes incubated for 60 mins by microbeta scintillation counting analysis B 8.26 pKi 5.5 nM Ki Eur J Med Chem (2019) 183: 111736-111736 [PMID:31586817]
ChEMBL Binding affinity against 5-hydroxytryptamine 1A human cloned receptors in HEK293 cells using [3H]8-OH-DPAT as radioligand B 8.4 pKi 3.98 nM Ki J. Med. Chem. (2003) 46: 5117-5120 [PMID:14613313]
ChEMBL Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor expressed in CHO-K1 cell membranes incubated for 60 mins by microbeta scintillation counting method B 8.44 pKi 3.6 nM Ki Eur J Med Chem (2019) 180: 383-397 [PMID:31325785]
ChEMBL In vitro inhibition of [3H]DPAT (1 nM) binding to 5-HT1A receptor from bovine hippocampus B 8.52 pKi 3 nM Ki J. Med. Chem. (1989) 32: 543-547 [PMID:2918500]
ChEMBL Displacement of [3H]-8-OH-DPAT from recombinant human 5HT1A receptor expressed in CHO cell membranes measured after 60 mins by microbeta scintillation counting analysis B 8.52 pKi 3 nM Ki Eur J Med Chem (2019) 166: 144-158 [PMID:30703658]
ChEMBL In vitro inhibition of [3H]DPAT (1 nM) binding to 5-hydroxytryptamine 1A receptor from bovine hippocampus B 8.55 pKi 2.8 nM Ki J. Med. Chem. (1989) 32: 543-547 [PMID:2918500]
ChEMBL The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1A receptor B 8.6 pKi 2.5 nM Ki J. Med. Chem. (1995) 38: 3602-3607 [PMID:7658447]
ChEMBL Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand B 8.61 pKi 2.48 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 1407-1412 [PMID:9871775]
ChEMBL Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1A receptor in CHO-K1 cells F 8.61 pKi 2.48 nM Ki J. Med. Chem. (1996) 39: 4920-4927 [PMID:8960551]
ChEMBL Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry B 8.68 pKi 2.08 nM Ki Eur. J. Med. Chem. (2014) 85: 716-726 [PMID:25128671]
ChEMBL Binding affinity was measured on 5-hydroxytryptamine 1A receptor in AK cells transfected with human 5-HT1A gene labeled with [3H]-8-OH-DPAT B 8.77 pKi 1.7 nM Ki J. Med. Chem. (1994) 37: 2828-2830 [PMID:8071931]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in CHO-K1 cell membranes after 60 mins by microbeta scintillation counting analysis B 8.85 pKi 1.4 nM Ki Bioorg Med Chem (2018) 26: 527-535 [PMID:29269256]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting B 8.89 pKi 1.3 nM Ki J Med Chem (2017) 60: 7483-7501 [PMID:28763213]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting method B 8.89 pKi 1.3 nM Ki Eur J Med Chem (2017) 137: 108-116 [PMID:28575721]
ChEMBL Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor B 8.9 pKi 1.26 nM Ki J. Med. Chem. (2008) 51: 2887-2890 [PMID:18433113]
ChEMBL Displacement of [3H]-8-OH-DPAT from human recombinant 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by microbeta2 scintillation counter B 8.92 pKi 1.2 nM Ki Bioorg Med Chem (2019) 27: 4163-4173 [PMID:31383628]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in CHOK1 cell membranes after 60 mins by microbeta scintillation counting method B 8.96 pKi 1.1 nM Ki MedChemComm (2017) 8: 1690-1696 [PMID:30108880]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry B 9.04 pKi 0.91 nM Ki Bioorg Med Chem Lett (2016) 26: 4052-4056 [PMID:27396505]
ChEMBL Displacement of [3H]8-OH-DPAT from 5-HT1A receptor (unknown origin) expressed in HEK293 cells by liquid scintillation counter B 9.05 pKi 0.9 nM Ki Bioorg. Med. Chem. (2013) 21: 856-868 [PMID:23332346]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells B 9.21 pKi 0.62 nM Ki Bioorg. Med. Chem. (2012) 20: 4862-4871 [PMID:22748706]
GtoPdb - - 9.7 pKi - - - Biochem J (1992) 285 ( Pt 3): 933-8 [PMID:1386736];
Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039];
Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 447-53 [PMID:10431754];
Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 205-17 [PMID:9550290];
Naunyn Schmiedebergs Arch Pharmacol (1997) 355: 682-8 [PMID:9205951];
Biosci Rep (2004) 24: 101-15 [PMID:15628665]
ChEMBL In vitro inhibition of [3H]5-HT (2 nM) binding to 5-hydroxytryptamine 1A receptor from bovine hippocampus B 8.22 pIC50 6 nM IC50 J. Med. Chem. (1989) 32: 543-547 [PMID:2918500]
ChEMBL In vitro inhibition of [3H]5-HT (2 nM) binding to 5-HT1A receptor from bovine hippocampus B 8.25 pIC50 5.6 nM IC50 J. Med. Chem. (1989) 32: 543-547 [PMID:2918500]
ChEMBL Binding affinity against 5-hydroxytryptamine 1A receptor B 8.28 pIC50 5.2 nM IC50 J. Med. Chem. (1992) 35: 4503-4505 [PMID:1447752]
ChEMBL In vitro inhibition of [125I]IPAPP (0.25 nM) binding to 5-HT1A receptor from bovine hippocampus B 8.7 pIC50 2 nM IC50 J. Med. Chem. (1989) 32: 543-547 [PMID:2918500]
ChEMBL In vitro inhibition of azido-[125I]-IPAPP (0.25 nM) binding to 5-HT1A receptor from bovine hippocampus B 8.7 pIC50 2 nM IC50 J. Med. Chem. (1989) 32: 543-547 [PMID:2918500]
ChEMBL In vitro inhibitory concentration required against [3H]8-OH-DPAT binding to cloned human 5-hydroxytryptamine 1A receptor B 8.92 pIC50 1.2 nM IC50 J. Med. Chem. (2003) 46: 4188-4195 [PMID:12954071]
ChEMBL Agonist activity at human 5HT1A receptor expressed in CHOK1 cells incubated for 16 hrs followed by forskolin-stimulation and measured after 2 hrs by dual-glo luciferase reporter gene assay B 5.74 pEC50 1800 nM EC50 J Nat Prod (2019) 82: 3302-3310 [PMID:31789520]
ChEMBL Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding F 6.64 pEC50 229.09