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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  • TA1 receptor/Trace amine-associated receptor 1 in Human [ChEMBL: CHEMBL5857] [GtoPdb: 364] [UniProtKB: Q96RJ0]
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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 Displacement of [3H]8-OH-DAPT from human recombinant 5-HT1A receptor expressed in CHO cells measured after 60 to 90 mins by radioligand completion assay relative to control B 8.35 pKi 4.5 nM Ki J Med Chem (2021) 64: 13510-13523 [PMID:34467758]
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 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-HT1A receptor from bovine hippocampus B 8.52 pKi 3 nM Ki J Med Chem (1989) 32: 543-547 [PMID:2918500]
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 nM EC50 J Med Chem (2007) 50: 5024-5033 [PMID:17803293]
ChEMBL Agonist activity at human 5-HT1A receptor expressed in CHO cells after 90 mins by beta-arrestin-2 recruitment assay B 6.77 pEC50 169.82 nM EC50 Bioorg Med Chem (2015) 23: 4824-4830 [PMID:26081758]
ChEMBL Agonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assay F 6.82 pEC50 150 nM EC50 Bioorg Med Chem (2009) 17: 4873-4880 [PMID:19559623]
ChEMBL Agonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding F 6.83 pEC50 147 nM EC50 J Med Chem (2010) 53: 1319-1328 [PMID:20041669]
ChEMBL Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay B 6.89 pEC50 128.82 nM EC50 J Med Chem (2020) 63: 10946-10971 [PMID:32883072]
ChEMBL Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay B 6.89 pEC50 128.82 nM EC50 J Med Chem (2019) 62: 2750-2771 [PMID:30721053]
ChEMBL Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay F 7.01 pEC50 97.7 nM EC50 Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027]
ChEMBL Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay F 7.16 pEC50 69.18 nM EC50 Eur J Med Chem (2017) 137: 108-116 [PMID:28575721]
ChEMBL Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay F 7.23 pEC50 58.88 nM EC50 J Med Chem (2020) 63: 10946-10971 [PMID:32883072]
ChEMBL Agonist activity at human recombinant 5-HT1A receptor expressed in CHOK1 cells measured after 1 hr by microbeta2 scintillation counter B 7.25 pEC50 56.23 nM EC50 Bioorg Med Chem (2019) 27: 4163-4173 [PMID:31383628]
ChEMBL Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay F 7.3 pEC50 50.12 nM EC50 J Med Chem (2019) 62: 2750-2771 [PMID:30721053]
ChEMBL Partial agonist activity at recombinant human 5-HT1A expressed in CHO-K1 cells by pathhunter beta-arrestin assay B 7.34 pEC50 45.3 nM EC50 Bioorg Med Chem Lett (2020) 30: 127358-127358 [PMID:32631554]
ChEMBL Compound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pig F 7.37 pEC50 43 nM EC50 Bioorg Med Chem Lett (1995) 5: 2391-2396
ChEMBL Agonist activity at 5HT1A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay B 7.41 pEC50 39 nM EC50 J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay B 7.48 pEC50 33.11 nM EC50 J Med Chem (2019) 62: 2750-2771 [PMID:30721053]
ChEMBL Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay B 7.48 pEC50 33.11 nM EC50 J Med Chem (2020) 63: 10946-10971 [PMID:32883072]
ChEMBL Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay F 7.51 pEC50 30.9 nM EC50 J Med Chem (2019) 62: 2750-2771 [PMID:30721053]
ChEMBL Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay F 7.51 pEC50 30.9 nM EC50 J Med Chem (2020) 63: 10946-10971 [PMID:32883072]
ChEMBL Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA F 7.56 pEC50 27.54 nM EC50 Bioorg Med Chem (2015) 23: 4824-4830 [PMID:26081758]
ChEMBL Agonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay F 7.72 pEC50 19 nM EC50 J Med Chem (2018) 61: 10017-10039 [PMID:30383372]
ChEMBL Agonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assay F 7.74 pEC50 18 nM EC50 Bioorg Med Chem Lett (2019) 29: 126703-126703 [PMID:31627993]
ChEMBL Agonist activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by Fluo-4 dye based FLIPR assay B 7.81 pEC50 15.33 nM EC50 Eur J Med Chem (2016) 123: 332-353 [PMID:27487565]
ChEMBL Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus. F 8 pEC50 10 nM EC50 J Med Chem (1992) 35: 4503-4505 [PMID:1447752]
ChEMBL Binding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-S F 8.06 pEC50 8.71 nM EC50 J Med Chem (2003) 46: 5117-5120 [PMID:14613313]
ChEMBL Agonist activity at human 5HT1A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay F 8.24 pEC50 5.8 nM EC50 Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805]
ChEMBL Agonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in calcium flux by fluorimetric method F 8.24 pEC50 5.7 nM EC50 Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL Agonist activity at human recombinant 5-HT1A receptor expressed in CHOK1 cells measured after 1 hr by microbeta2 scintillation counter B 8.25 pEC50 5.61 nM EC50 Bioorg Med Chem (2019) 27: 4163-4173 [PMID:31383628]
ChEMBL Agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay F 8.43 pEC50 3.75 nM EC50 Bioorg Med Chem (2013) 21: 856-868 [PMID:23332346]
ChEMBL Tested for functional response on CHO cells expressing cloned human 5-hydroxytryptamine 1A receptor B 8.43 pEC50 3.7 nM EC50 J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
ChEMBL Agonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assay F 8.52 pEC50 3 nM EC50 Bioorg Med Chem (2014) 22: 5838-5846 [PMID:25308766]
ChEMBL Agonist activity at human 5-HT1A receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay F 8.69 pEC50 2.03 nM EC50 Eur J Med Chem (2021) 214: 113243-113243 [PMID:33582388]
ChEMBL Agonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulation F 9 pEC50 1 nM EC50 J Med Chem (2006) 49: 125-134 [PMID:16392798]
ChEMBL Agonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cells F 9.15 pEC50 0.7 nM EC50 Bioorg Med Chem Lett (2006) 16: 2101-2104 [PMID:16458504]
ChEMBL Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding F 9.3 pEC50 0.5 nM EC50 J Med Chem (2006) 49: 125-134 [PMID:16392798]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264]
ChEMBL Inhibitory activity towards 5-hydroxytryptamine 1A receptor by the displacement of [3H]8-OH-DPAT in mouse hippocampus B 8.3 pIC50 5 nM IC50 J Med Chem (1990) 33: 386-394 [PMID:2136918]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Displacement of [3H]8-OH-DPAT from 5HT1A receptor in Rattus norvegicus (rat) cerebral cortex after 15 min by filter binding assay B 8.05 pKi 9 nM Ki Med Chem Res (2008) 17: 507-514
ChEMBL Ability to displace [3H]- -(OH)-DPAT bound to 5-hydroxytryptamine 1A receptor in rat hippocampus B 8.14 pKi 7.3 nM Ki J Med Chem (1998) 41: 728-741 [PMID:9513601]
ChEMBL Binding affinity against 5-hydroxytryptamine 1A receptor of rat hippocampus tissue. B 8.14 pKi 7.3 nM Ki J Med Chem (1999) 42: 1556-1575 [PMID:10229626]
ChEMBL Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement B 8.32 pKi 4.79 nM Ki J Med Chem (1996) 39: 126-134 [PMID:8568799]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor by the displacement of [125I]trans-8-OH-PIPAT in membrane homogenates of hippocampal tissue of rat brain B 8.37 pKi 4.31 nM Ki J Med Chem (1993) 36: 3161-3165 [PMID:8230102]
ChEMBL Displacement of [3H]8-OH-DPAT from rat 5HT1A receptor expressed in CHO cells B 8.52 pKi 3 nM Ki Bioorg Med Chem (2008) 16: 6675-6681 [PMID:18562201]
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 8.52 pKi 3 nM Ki J Med Chem (1987) 30: 1-12 [PMID:3543362]
ChEMBL Displacement of [3H]8OH-DPAT from 5HT1A in rat brain cerebral cortex after 15 mins by scintillation counting B 8.59 pKi 2.6 nM Ki Eur J Med Chem (2011) 46: 4474-4488 [PMID:21816515]
ChEMBL Displacement of [3H]-8-OH-DPAT from rat cerebral cortex 5HT1A receptor measured after 15 mins by liquid scintillation counter method B 8.64 pKi 2.3 nM Ki Bioorg Med Chem (2016) 24: 3994-4007 [PMID:27377863]
ChEMBL The compound was tested for their binding affinity towards 5-hydroxytryptamine 1A receptor from rat hippocampus using [3H]8-OH-DPAT as radioligand. B 8.68 pKi 2.1 nM Ki J Med Chem (1995) 38: 2692-2704 [PMID:7629808]
ChEMBL Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in rat hippocampal membranes after 20 mins B 8.68 pKi 2.1 nM Ki Eur J Med Chem (2013) 63: 484-500 [PMID:23524160]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 1A receptor was determined in male Sprague-Dawley rat brain. B 8.7 pKi 2 nM Ki J Med Chem (1990) 33: 755-758 [PMID:2299641]
ChEMBL Binding affinity to 5HT1A receptor in rat cortex membrane B 8.73 pKi 1.86 nM Ki J Med Chem (2007) 50: 5024-5033 [PMID:17803293]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor B 8.77 pKi 1.7 nM Ki J Med Chem (1988) 31: 867-870 [PMID:2965244]
ChEMBL Displacement of [3H]8-OHDPAT from 5HT1A receptor in rat hippocampus B 8.8 pKi 1.6 nM Ki J Med Chem (2009) 52: 6946-6950 [PMID:19831400]
ChEMBL Displacement of [3H]8-OHDPAT from 5HT1A receptor in rat hippocampus B 8.8 pKi 1.6 nM Ki J Med Chem (2009) 52: 3548-3562 [PMID:19425598]
ChEMBL The compound was tested for the binding affinity against 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand. B 8.8 pKi 1.58 nM Ki J Med Chem (1999) 42: 4362-4379 [PMID:10543880]
ChEMBL Displacement of [3H]8-OH-DPAT from rat cortex 5-hydroxytryptamine 1A receptor B 8.28 pIC50 5.2 nM IC50 J Med Chem (1990) 33: 2087-2093 [PMID:2374139]
ChEMBL Binding affinity was measured against serotonin 5-hydroxytryptamine 1A receptor B 8.28 pIC50 5.2 nM IC50 J Med Chem (1994) 37: 2509-2512 [PMID:8057297]
ChEMBL Tested in vitro for receptor binding affinity to 5-hydroxytryptamine 1A receptor in rat cortex using [3H]OH-DPAT radioligand B 8.28 pIC50 5.2 nM IC50 Bioorg Med Chem Lett (1995) 5: 2391-2396
ChEMBL In vitro inhibitory concentration against radioligand [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor in rat hippocampal membrane. B 8.52 pIC50 3 nM IC50 J Med Chem (1997) 40: 574-585 [PMID:9046348]
ChEMBL Inhibition of radiolabeled [3H]-8-OH-DPAT ligand binding to 5-hydroxytryptamine 1A receptor B 8.59 pIC50 2.6 nM IC50 J Med Chem (1997) 40: 3670-3678 [PMID:9357534]
ChEMBL Agonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS binding F 6.49 pEC50 323 nM EC50 J Med Chem (2008) 51: 4529-4538 [PMID:18598015]
ChEMBL Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor F 8 pEC50 10 nM EC50 J Med Chem (1994) 37: 2509-2512 [PMID:8057297]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 8.4 pKd - - - Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658];
J Neurochem (1996) 67: 2096-103 [PMID:8863519]
ChEMBL Displacement of radiolabeled serotonin from human 5HT1B receptor B 7.74 pKi 18 nM Ki J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Displacement of [125I]CYP from human 5HT1B receptor B 7.85 pKi 14 nM Ki J Med Chem (2011) 54: 5320-5334 [PMID:21726069]
ChEMBL The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta B 8.15 pKi 7.1 nM Ki J Med Chem (1995) 38: 3602-3607 [PMID:7658447]
ChEMBL Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells F 8.17 pKi 6.76 nM Ki J Med Chem (1996) 39: 4920-4927 [PMID:8960551]
ChEMBL Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand B 8.17 pKi 6.76 nM Ki Bioorg Med Chem Lett (1998) 8: 1407-1412 [PMID:9871775]
ChEMBL Binding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligand B 8.3 pKi 5.01 nM Ki J Med Chem (2003) 46: 5117-5120 [PMID:14613313]
ChEMBL Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor B 8.32 pKi 4.8 nM Ki J Med Chem (2003) 46: 265-283 [PMID:12519065]
ChEMBL Binding affinity to human 5-HT1B receptor by radioligand displacement assay B 8.4 pKi 4 nM Ki Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL Binding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined using [3H]8-OH-DPAT as radioligand B 8.4 pKi 4 nM Ki J Med Chem (1996) 39: 314-322 [PMID:8568822]
ChEMBL Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT B 8.4 pKi 4 nM Ki J Med Chem (1994) 37: 2828-2830 [PMID:8071931]
ChEMBL Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting B 8.96 pKi 1.1 nM Ki J Med Chem (2008) 51: 3609-3616 [PMID:18507369]
GtoPdb - - 9 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 447-53 [PMID:10431754];
Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658];
Br J Pharmacol (1997) 121: 737-42 [PMID:9208142];
Br J Pharmacol (1998) 125: 202-8 [PMID:9776361];
Mol Pharmacol (2000) 58: 1042-9 [PMID:11040052];
Eur J Pharmacol (1996) 314: 365-72 [PMID:8957260]
ChEMBL Displacement of radiolabeled serotonin from human 5HT1B receptor B 7.54 pIC50 29 nM IC50 J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Inhibition of 5HT1B receptor B 7.8 pIC50 16 nM IC50 J Med Chem (2008) 51: 4150-4169 [PMID:18588282]
ChEMBL Binding affinity to 5-HT1B receptor (unknown origin) by radioligand displacement assay B 7.92 pIC50 12 nM IC50 Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL Binding affinity to human 5-HT1B receptor by radioligand displacement assay B 8.19 pIC50 6.5 nM IC50 Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL Binding affinity against 5-hydroxytryptamine 1B receptor B 8.3 pIC50 5 nM IC50 J Med Chem (1992) 35: 4503-4505 [PMID:1447752]
ChEMBL Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampus B 7.52 pEC50 30 nM EC50 J Med Chem (1990) 33: 2087-2093 [PMID:2374139]
ChEMBL Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells F 8.32 pEC50 4.82 nM EC50 J Med Chem (1996) 39: 4920-4927 [PMID:8960551]
ChEMBL The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full Agonist F 8.33 pEC50 4.67 nM EC50 Bioorg Med Chem Lett (1998) 8: 1407-1412 [PMID:9871775]
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 7.6 pKi 25 nM Ki J Med Chem (1987) 30: 1-12 [PMID:3543362]
ChEMBL Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptor B 8.27 pKi 5.4 nM Ki J Med Chem (1988) 31: 867-870 [PMID:2965244]
ChEMBL Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT B 8.27 pKi 5.4 nM Ki J Med Chem (1994) 37: 2828-2830 [PMID:8071931]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain. B 8.3 pKi 5 nM Ki J Med Chem (1990) 33: 755-758 [PMID:2299641]
ChEMBL Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate B 8.46 pKi 3.47 nM Ki J Med Chem (1988) 31: 1406-1412 [PMID:3385733]
ChEMBL The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand. B 8.6 pKi 2.51 nM Ki J Med Chem (1999) 42: 4362-4379 [PMID:10543880]
ChEMBL The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand. B 8.6 pKi 2.5 nM Ki J Med Chem (1995) 38: 2692-2704 [PMID:7629808]
ChEMBL Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum B 8.96 pKi 1.1 nM Ki J Med Chem (1998) 41: 728-741 [PMID:9513601]
ChEMBL Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum. B 8.96 pKi 1.1 nM Ki J Med Chem (1999) 42: 1556-1575 [PMID:10229626]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand. B 8.3 pIC50 5 nM IC50 J Med Chem (1990) 33: 2087-2093 [PMID:2374139]
ChEMBL Displacement of [125I]CYP from rat cerebral cortex 5-HT1B receptor in the presence of isoproternol B 8.31 pIC50 4.9 nM IC50 Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL Displacement of [125I]CYP from rat cerebral cortex 5HT1B receptor measured after 120 mins by scintillation counting method B 8.31 pIC50 4.9 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor B 8.34 pIC50 4.6 nM IC50 J Med Chem (1997) 40: 3670-3678 [PMID:9357534]
ChEMBL Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra B 7.59 pEC50 26 nM EC50 J Med Chem (1990) 33: 2087-2093 [PMID:2374139]
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 7.9 pKd 7.9 - pKD J Med Chem (1993) 36: 1918-1919 [PMID:8515429]
ChEMBL Binding affinity was measured on 5-hydroxytryptamine 1D receptor alpha in COS cells transfected with human 5-HT1D alpha gene labeled with [3H]5-HT B 8.26 pKi 5.5 nM Ki J Med Chem (1994) 37: 2828-2830 [PMID:8071931]
ChEMBL Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1D receptor using [3H]-5-CT as radioligand B 8.3 pKi 5.06 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 1D receptor in CHO-K1 cells F 8.3 pKi 5.06 nM Ki J Med Chem (1996) 39: 4920-4927 [PMID:8960551]
ChEMBL Binding affinity to recombinant human 5-hydroxytryptamine 1D receptor alpha B 8.32 pKi 4.8 nM Ki J Med Chem (1995) 38: 3602-3607 [PMID:7658447]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 1D receptor in bovine caudate homogenate B 8.52 pKi 3 nM Ki J Med Chem (1990) 33: 755-758 [PMID:2299641]
ChEMBL In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1D receptor B 8.7 pKi 2 nM Ki J Med Chem (1999) 42: 526-531 [PMID:9986723]
ChEMBL In vitro affinity human cloned 5-hydroxytryptamine 1D receptor alpha by [3H]5-HT displacement. B 8.77 pKi 1.7 nM Ki J Med Chem (1996) 39: 314-322 [PMID:8568822]
GtoPdb - - 9 pKi - - - Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658];
Br J Pharmacol (1997) 121: 737-42 [PMID:9208142];
Br J Pharmacol (1998) 125: 202-8 [PMID:9776361];
Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 447-53 [PMID:10431754];
Mol Pharmacol (1996) 50: 1567-80 [PMID:8967979];
Eur J Pharmacol (1996) 314: 365-72 [PMID:8957260];
Mol Pharmacol (1991) 40: 143-8 [PMID:1652050]
ChEMBL Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1D receptor expressed in CHOK1 cells by liquid scintillation counting B 9.3 pKi 0.5 nM Ki J Med Chem (2008) 51: 3609-3616 [PMID:18507369]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 1D receptor of bovine caudate using [3H]5-HT as the radioligand B 8.52 pIC50 3 nM IC50 J Med Chem (1990) 33: 2087-2093 [PMID:2374139]
ChEMBL Tested in vitro for receptor binding affinity to 5-hydroxytryptamine 1D receptor in bovine caudate using [3H]5-HT radioligand B 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (1995) 5: 2391-2396
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 pIC50 10 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 pIC50 10 nM IC50 J Med Chem (1993) 36: 1529-1538 [PMID:8496922]
ChEMBL Compound was tested for the displacement of [3H]-5-HT to 5-hydroxytryptamine 1D receptor recognition sites in pig caudate membranes B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (1993) 3: 993-997
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5450] [GtoPdb: 3] [UniProtKB: P28565]
ChEMBL Binding affinity was measured against serotonin 5-hydroxytryptamine 1D receptor B 8.52 pIC50 3 nM IC50 J Med Chem (1994) 37: 2509-2512 [PMID:8057297]
ChEMBL Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1D receptor F 8.28 pEC50 5.2 nM EC50 J Med Chem (1994) 37: 2509-2512 [PMID:8057297]
Serotonin 1d (5-HT1d) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304407] [UniProtKB: Q60484]
ChEMBL Binding affinity against 5-hydroxytryptamine 1D receptor B 8.52 pIC50 3 nM IC50 J Med Chem (1992) 35: 4503-4505 [PMID:1447752]
ChEMBL Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1D receptor of guinea pig substantia nigra B 7.8 pEC50 16 nM EC50 J Med Chem (1990) 33: 2087-2093 [PMID:2374139]
ChEMBL Compound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1D receptor in guinea pig substantia nigra B 8.07 pEC50 8.5 nM EC50 Bioorg Med Chem Lett (1995) 5: 2391-2396
ChEMBL Effect on forskolin stimulated adenylate cyclase activity at 5-HT1D receptor of guinea pig substantia nigra. F 8.28 pEC50 5.2 nM EC50 J Med Chem (1992) 35: 4503-4505 [PMID:1447752]
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
ChEMBL Displacement of [3H]5HT from 5-HT1E receptor (unknown origin) B 7.96 pKi 11 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]5HT from 5-HT1E receptor (unknown origin) B 7.97 pKi 10.72 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
GtoPdb - - 8.2 pKi - - - 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];
Bioorg Med Chem (2004) 12: 2545-52 [PMID:15110837]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 1E receptor in human cortical homogenate B 8.4 pKi 4 nM Ki J Med Chem (1990) 33: 755-758 [PMID:2299641]
5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939]
GtoPdb - - 8 pKd - - - Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]
GtoPdb - - 8 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2005) 371: 169-77 [PMID:15900510];
Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639];
Neuropharmacology (1997) 36: 569-76 [PMID:9225282]
ChEMBL In vitro effective concentration for inhibition of skolin-stimulated adenylate cyclase in cell line expressing human 5-hydroxytryptamine 1F receptor F 8.1 pEC50 7.9 nM EC50 J Med Chem (2001) 44: 4031-4034 [PMID:11708905]
5-HT1F receptor in Rat [GtoPdb: 5] [UniProtKB: P30940]
GtoPdb - - 7.2 pIC50 - - - Proc Natl Acad Sci USA (1993) 90: 2184-8 [PMID:8384716]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 8.9 pKd - - - Biochem Pharmacol (1996) 51: 71-6 [PMID:8534270]
ChEMBL Displacement of [N-methyl-3H]LSD from human 5HT2A receptor expressed in HEK293 cells B 6.16 pKi 690 nM Ki J Nat Prod (2006) 69: 1421-1424 [PMID:17067154]
ChEMBL Binding affinity was measured on 5-hydroxytryptamine 2A receptor in GF6 cells transfected with human 5-HT2A gene labeled with [3H]ketanserin B 6.29 pKi 510 nM Ki J Med Chem (1994) 37: 2828-2830 [PMID:8071931]
ChEMBL Binding affinity against 5-hydroxytryptamine 2A receptor human cloned receptors in HEK 293 cells using [3H]ketanserin as radioligand B 6.4 pKi 398.11 nM Ki J Med Chem (2003) 46: 5117-5120 [PMID:14613313]
ChEMBL Displacement of [3H]ketanserin from human 5HT2A receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis B 6.49 pKi 323.59 nM Ki J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL Displacement of [3H]methylspiperone form human cloned 5HT2A receptor expressed in african green monkey COS7 cells by scintillation spectroscopy B 6.49 pKi 320 nM Ki J Nat Prod (2002) 65: 476-480 [PMID:11975483]
ChEMBL Displacement of [3H]ketanserin from human 5HT2A receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis B 6.49 pKi 320 nM Ki J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL Displacement of [3H]INBMeO from human 5HT2A receptor expressed in human A549 cells B 6.8 pKi 160 nM Ki Bioorg Med Chem (2008) 16: 6116-6123 [PMID:18468904]
ChEMBL Displacement of [3H]INBMeO from human 5HT2A receptor expressed in human HEK293 cells B 6.82 pKi 150 nM Ki Bioorg Med Chem (2008) 16: 6116-6123 [PMID:18468904]
ChEMBL Displacement of [3H]ketanserin from human 5HT2A receptor expressed in human HEK293 cells B 6.89 pKi 130 nM Ki Bioorg Med Chem (2008) 16: 6116-6123 [PMID:18468904]
ChEMBL Displacement of [3H]ketanserin from human 5HT2A receptor expressed in human A549 cells B 6.92 pKi 120 nM Ki Bioorg Med Chem (2008) 16: 6116-6123 [PMID:18468904]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT2A receptor expressed in HEK cells by radioligand completion assay relative to control B 7.76 pKi 17.2 nM Ki J Med Chem (2021) 64: 13510-13523 [PMID:34467758]
ChEMBL Displacement of [125I]DOI from human 5HT2A B 7.85 pKi 14 nM Ki Bioorg Med Chem Lett (2006) 16: 677-680 [PMID:16257207]
ChEMBL Affinity for human 5-hydroxytryptamine 2A receptor expressed in mammalian cell line B 7.85 pKi 14 nM Ki Bioorg Med Chem Lett (2004) 14: 2367-2370 [PMID:15081042]
ChEMBL Displacement of [125I]DOI from human 5HT2A receptor expressed in HEK293 cell membranes B 7.94 pKi 11.5 nM Ki J Med Chem (2018) 61: 9121-9131 [PMID:30240563]
ChEMBL Displacement of [125I]DOI from cloned human 5HT2A receptor expressed in CHO cells B 8.09 pKi 8.2 nM Ki J Med Chem (2006) 49: 318-328 [PMID:16392816]
ChEMBL Inhibitory constant against cloned human 5-hydroxytryptamine 2A receptor using with [125I]- DOI radioligand B 8.09 pKi 8.2 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
GtoPdb - - 8.4 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733];
Biochem Pharmacol (1996) 51: 71-6 [PMID:8534270];
J Med Chem (2003) 46: 4188-95 [PMID:12954071];
Mol Pharmacol (1990) 38: 604-9 [PMID:2233697];
Mol Pharmacol (1994) 45: 277-86 [PMID:8114677];
J Biol Chem (1996) 271: 14672-5 [PMID:8663249]
ChEMBL Antagonist activity at recombinant human 5-HT2A expressed in human U2OS cells by pathhunter beta-arrestin assay B 7.55 pIC50 27.9 nM IC50 Bioorg Med Chem Lett (2020) 30: 127358-127358 [PMID:32631554]
ChEMBL Partial agonist activity at human 5-HT2A receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assay B 6.52 pEC50 302 nM EC50 Bioorg Med Chem (2015) 23: 3933-3937 [PMID:25583099]
ChEMBL Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay F 6.82 pEC50 150 nM EC50 J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay F 6.83 pEC50 147.91 nM EC50 J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation F 6.9 pEC50 125.89 nM EC50 J Med Chem (2008) 51: 305-313 [PMID:18095642]
ChEMBL Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis F 7.15 pEC50 70 nM EC50 Bioorg Med Chem (2008) 16: 1966-1982 [PMID:18035544]
ChEMBL Agonist activity at 5-HT2A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by Fluo-4 dye based FLIPR assay B 7.33 pEC50 47 nM EC50 Eur J Med Chem (2016) 123: 332-353 [PMID:27487565]
ChEMBL Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay B 7.73 pEC50 18.62 nM EC50 US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)
ChEMBL Agonist activity at 5HT2A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay B 7.8 pEC50 16 nM EC50 J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL Binding to human 5HT2A receptor expressed in CHO cells B 7.96 pEC50 11 nM EC50 Bioorg Med Chem Lett (2006) 16: 677-680 [PMID:16257207]
ChEMBL Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader F 7.96 pEC50 11 nM EC50 Bioorg Med Chem Lett (2004) 14: 2367-2370 [PMID:15081042]
ChEMBL Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay F 8.12 pEC50 7.6 nM EC50 ACS Med Chem Lett (2011) 2: 929-932 [PMID:22778800]
ChEMBL Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay F 8.24 pEC50 5.8 nM EC50 J Med Chem (2009) 52: 1885-1902 [PMID:19284718]
ChEMBL Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay F 8.59 pEC50 2.6 nM EC50 J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay F 8.59 pEC50 2.57 nM EC50 J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay F 8.63 pEC50 2.35 nM EC50 J Med Chem (2016) 59: 9866-9880 [PMID:27726356]
ChEMBL Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay F 8.63 pEC50 2.34 nM EC50 J Med Chem (2016) 59: 9866-9880 [PMID:27726356]
ChEMBL Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay F 8.73 pEC50 1.88 nM EC50 J Med Chem (2015) 58: 1992-2002 [PMID:25633969]
ChEMBL Agonist activity at serotonin 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay F 8.8 pEC50 1.6 nM EC50 J Med Chem (2018) 61: 10017-10039 [PMID:30383372]
ChEMBL Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay F 8.81 pEC50 1.55 nM EC50 Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay F 8.82 pEC50 1.5 nM EC50 Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL Agonist activity at human 5HT2A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay F 8.96 pEC50 1.1 nM EC50 Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805]
ChEMBL Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay F 9.29 pEC50 0.51 nM EC50 J Nat Prod (2020) 83: 461-467 [PMID:32077284]
ChEMBL Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay F 9.29 pEC50 0.51 nM EC50 J Nat Prod (2020) 83: 461-467 [PMID:32077284]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5377] [GtoPdb: 6] [UniProtKB: P35363]
ChEMBL Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay F 9.28 pEC50 0.53 nM EC50 J Nat Prod (2020) 83: 461-467 [PMID:32077284]
ChEMBL Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay F 9.28 pEC50 0.52 nM EC50 J Nat Prod (2020) 83: 461-467 [PMID:32077284]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL The compound was tested for the binding affinity against 5-hydroxytryptamine 2A receptor using [3H]ketanserin as radioligand. B 5.9 pKi 1258.93 nM Ki J Med Chem (1999) 42: 4362-4379 [PMID:10543880]
ChEMBL Displacement of [3H]ketanserin from 5HT2A receptor in rat cortex B 5.9 pKi 1258 nM Ki J Med Chem (2009) 52: 3548-3562 [PMID:19425598]
ChEMBL Displacement of [3H]ketanserin from 5HT2A receptor in rat cortex B 5.9 pKi 1258 nM Ki J Med Chem (2009) 52: 6946-6950 [PMID:19831400]
ChEMBL Displacement of [3H]ketanserin from 5HT2A in Sprague-Dawley rat frontal cortex membranes measured after 20 mins B 6.22 pKi 600 nM Ki J Med Chem (2017) 60: 2605-2628 [PMID:28244748]
GtoPdb - - 6.5 pKi - - - Mol Pharmacol (2000) 58: 877-86 [PMID:11040033];
Circulation (2000) 102: 2836-41 [PMID:11104741];
J Pharmacol Exp Ther (1998) 286: 85-90 [PMID:9655845]
ChEMBL Displacement of [3H]DOI-HCL from 5HT2A in Sprague-Dawley rat frontal cortex membranes measured after 20 mins B 7.97 pKi 10.6 nM Ki J Med Chem (2017) 60: 2605-2628 [PMID:28244748]
ChEMBL In vitro inhibitory constant against [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex B 9.52 pKi 0.3 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
ChEMBL Displacement of [3H]-ketanserin from 5HT2A receptor low affinity component in rat brain cortical membranes after 15 mins by competition assay B 4.51 pIC50 30600 nM IC50 Eur J Med Chem (2013) 66: 122-134 [PMID:23792350]
ChEMBL Displacement of [3H]-ketanserin from 5HT2A receptor in rat brain cortical membranes after 15 mins by competition assay in presence of Gpp(NH)p B 4.89 pIC50 13000 nM IC50 Eur J Med Chem (2013) 66: 122-134 [PMID:23792350]
ChEMBL Inhibition of radiolabeled [3H]-Ketanserin ligand binding to 5-hydroxytryptamine 2A receptor B 5.63 pIC50 2350 nM IC50 J Med Chem (1997) 40: 3670-3678 [PMID:9357534]
ChEMBL Displacement of [3H]-ketanserin from 5HT2A receptor high affinity component in rat brain cortical membranes after 15 mins by competition assay B 6.22 pIC50 600 nM IC50 Eur J Med Chem (2013) 66: 122-134 [PMID:23792350]
ChEMBL Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex B 9.03 pIC50 0.94 nM IC50 J Med Chem (2006) 49: 318-328 [PMID:16392816]
ChEMBL In vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex B 9.05 pIC50 0.9 nM IC50 J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
ChEMBL In vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cells F 6.45 pEC50 351 nM EC50 J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
ChEMBL Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells F 7.24 pEC50 57.9 nM EC50 J Med Chem (2006) 49: 318-328 [PMID:16392816]
ChEMBL The receptor (5-hydroxytryptamine 2A ) mediated mobilization of intracellular calcium [Ca2+] was studied in rat smooth muscle cells F 7.25 pEC50 55.8 nM EC50 J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) B 7.87 pKi 13.49 nM Ki Bioorg Med Chem Lett (2014) 24: 1489-1492 [PMID:24582985]
ChEMBL Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand B 7.89 pKi 13 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
ChEMBL Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells B 7.89 pKi 13 nM Ki J Med Chem (2006) 49: 318-328 [PMID:16392816]
ChEMBL Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line B 7.92 pKi 12 nM Ki Bioorg Med Chem Lett (2004) 14: 2367-2370 [PMID:15081042]
ChEMBL Displacement of [3H]5-HT from human 5HT2B B 7.92 pKi 12 nM Ki Bioorg Med Chem Lett (2006) 16: 677-680 [PMID:16257207]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control B 7.97 pKi 10.8 nM Ki J Med Chem (2021) 64: 13510-13523 [PMID:34467758]
GtoPdb - - 8.4 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733];
J Med Chem (2003) 46: 4188-95 [PMID:12954071];
Circulation (2000) 102: 2836-41 [PMID:11104741];
Mol Pharmacol (1994) 46: 227-34 [PMID:8078486];
Br J Pharmacol (2004) 143: 549-60 [PMID:15466450]
ChEMBL Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation F 7.6 pEC50 25.12 nM EC50 J Med Chem (2008) 51: 305-313 [PMID:18095642]
ChEMBL Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay F 7.96 pEC50 11 nM EC50 Bioorg Med Chem Lett (2009) 19: 4999-5003 [PMID:19646865]
ChEMBL Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis F 8.24 pEC50 5.8 nM EC50 Bioorg Med Chem (2008) 16: 1966-1982 [PMID:18035544]
ChEMBL Agonist activity at human 5-HT2BR expressed in CHO cells assessed as induction of IP1 accumulation after 30 mins by HTRF method F 8.35 pEC50 4.5 nM EC50 Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL Binding to human 5HT2B receptor expressed in CHO cells B 8.82 pEC50 1.5 nM EC50 Bioorg Med Chem Lett (2006) 16: 677-680 [PMID:16257207]
ChEMBL Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader F 8.82 pEC50 1.5 nM EC50 Bioorg Med Chem Lett (2004) 14: 2367-2370 [PMID:15081042]
ChEMBL Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay F 8.84 pEC50 1.46 nM EC50 J Med Chem (2016) 59: 9866-9880 [PMID:27726356]
ChEMBL Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay F 8.84 pEC50 1.45 nM EC50 J Med Chem (2016) 59: 9866-9880 [PMID:27726356]
ChEMBL Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay F 8.96 pEC50 1.1 nM EC50 Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay F 8.97 pEC50 1.07 nM EC50 Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay F 9.04 pEC50 0.92 nM EC50 J Med Chem (2015) 58: 1992-2002 [PMID:25633969]
ChEMBL Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay F 9.07 pEC50 0.86 nM EC50 ACS Med Chem Lett (2011) 2: 929-932 [PMID:22778800]
ChEMBL Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay F 9.3 pEC50 0.5 nM EC50 J Med Chem (2009) 52: 1885-1902 [PMID:19284718]
ChEMBL Agonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assay F 10.15 pEC50 0.07 nM EC50 Bioorg Med Chem Lett (2020) 30: 127511-127511 [PMID:32853682]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994]
GtoPdb - - 8 pKi - - - Mol Pharmacol (1993) 43: 419-26 [PMID:8450835]
ChEMBL Agonist activity at 5HT2b receptor in Wistar rat fundus measured for 90 secs B 8.38 pEC50 4.19 nM EC50 Eur J Med Chem (2015) 103: 289-301 [PMID:26363507]
ChEMBL Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats F 8.46 pEC50 3.5 nM EC50 J Med Chem (2006) 49: 318-328 [PMID:16392816]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Displacement of [3H]-mesulergine from 5HT2C receptor expressed in CHO cell membranes using 11 concentration of ligand after 90 mins by scintillation counting using complete competition binding curves analysis B 6.35 pKi 445 nM Ki Bioorg Med Chem Lett (2012) 22: 2560-2564 [PMID:22381048]
ChEMBL Displacement of [3H]-mesulergine from 5HT2C receptor expressed in CHO cell membranes after 90 mins by scintillation counting B 6.67 pKi 214 nM Ki Bioorg Med Chem Lett (2012) 22: 2560-2564 [PMID:22381048]
ChEMBL Displacement of [3H]mesulergine form human cloned 5HT2C receptor expressed in african green monkey COS7 cells by scintillation spectroscopy B 6.89 pKi 130 nM Ki J Nat Prod (2002) 65: 476-480 [PMID:11975483]
ChEMBL Displacement of [3H]mesulergine from human 5HT2C receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis B 7.1 pKi 79.43 nM Ki J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL Displacement of [3H]mesulergine from human 5HT2C receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis B 7.1 pKi 79 nM Ki J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL Binding affinity against 5-hydroxytryptamine 2C receptor human cloned receptors in HEK 293 cells using [3H]mesulergine as radioligand B 7.3 pKi 50.12 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 7.46 pKi 35 nM Ki J Med Chem (1987) 30: 1-12 [PMID:3543362]
ChEMBL Displacement of [N-methyl-3H]LSD from human 5HT2C receptor expressed in HEK293 cells B 7.7 pKi 20 nM Ki J Nat Prod (2006) 69: 1421-1424 [PMID:17067154]
ChEMBL Inhibitory constant against cloned human 5-hydroxytryptamine 2C receptor using with [125I]- DOI radioligand B 8.08 pKi 8.3 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
ChEMBL Displacement of [125I]DOI from cloned human 5HT2C receptor expressed in CHO cells B 8.08 pKi 8.3 nM Ki J Med Chem (2006) 49: 318-328 [PMID:16392816]
ChEMBL Affinity for human 5-hydroxytryptamine 2C receptor expressed in mammalian cell line B 8.16 pKi 6.9 nM Ki Bioorg Med Chem Lett (2004) 14: 2367-2370 [PMID:15081042]
ChEMBL Displacement of [3H]5-HT from human 5HT2C B 8.16 pKi 6.9 nM Ki Bioorg Med Chem Lett (2006) 16: 677-680 [PMID:16257207]
GtoPdb - - 8.6 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733];
J Med Chem (2003) 46: 4188-95 [PMID:12954071];
J Neurochem (1999) 72: 2127-34 [PMID:10217294];
Synapse (2000) 35: 144-150 [PMID:10611640];
Eur J Pharmacol (2004) 483: 37-43 [PMID:14709324]
ChEMBL inhibitory activity against 5-hydroxytryptamine 1C receptor of pig choroid plexus using [3H]mesulergine as the radioligand B 7.09 pIC50 81 nM IC50 J Med Chem (1990) 33: 2087-2093 [PMID:2374139]
ChEMBL Antagonist activity at recombinant human 5-HT2C expressed in human U2OS cells by pathhunter beta-arrestin assay B 8.9 pIC50 1.25 nM IC50 Bioorg Med Chem Lett (2020) 30: 127358-127358 [PMID:32631554]
ChEMBL Partial agonist activity at human 5-HT2C receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assay B 6.72 pEC50 190.55 nM EC50 Bioorg Med Chem (2015) 23: 3933-3937 [PMID:25583099]
ChEMBL Agonist activity at 5HT2C receptor VGV isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay B 7.29 pEC50 51.29 nM EC50 US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)
ChEMBL Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay F 7.36 pEC50 44 nM EC50 J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay F 7.36 pEC50 43.65 nM EC50 J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation F 7.6 pEC50 25.12 nM EC50 J Med Chem (2008) 51: 305-313 [PMID:18095642]
ChEMBL Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as induction of calcium mobilization by FLIPR assay F 7.6 pEC50 25 nM EC50 Bioorg Med Chem Lett (2009) 19: 4999-5003 [PMID:19646865]
ChEMBL Agonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis F 7.62 pEC50 24 nM EC50 Bioorg Med Chem (2008) 16: 1966-1982 [PMID:18035544]
ChEMBL Agonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assay B 7.66 pEC50 21.88 nM EC50 J Med Chem (2016) 59: 9866-9880 [PMID:27726356]
ChEMBL Agonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assay B 7.68 pEC50 21 nM EC50 J Med Chem (2016) 59: 9866-9880 [PMID:27726356]
ChEMBL Agonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assay B 7.82 pEC50 15.14 nM EC50 J Med Chem (2017) 60: 6273-6288 [PMID:28657744]
ChEMBL Agonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assay B 7.82 pEC50 15 nM EC50 J Med Chem (2017) 60: 6273-6288 [PMID:28657744]
ChEMBL Functional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate reader F 8.77 pEC50 1.7 nM EC50 Bioorg Med Chem Lett (2004) 14: 2367-2370 [PMID:15081042]
ChEMBL Binding to human 5HT2C receptor expressed in CHO cells B 8.77 pEC50 1.7 nM EC50 Bioorg Med Chem Lett (2006) 16: 677-680 [PMID:16257207]
ChEMBL Agonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assay F 8.79 pEC50 1.63 nM EC50 Bioorg Med Chem Lett (2012) 22: 2560-2564 [PMID:22381048]
ChEMBL Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay F 9.06 pEC50 0.87 nM EC50 J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay F 9.06 pEC50 0.87 nM EC50 J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL Agonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assay F 9.39 pEC50 0.41 nM EC50 J Med Chem (2020) 63: 4579-4602 [PMID:32282200]
ChEMBL Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay F 9.4 pEC50 0.4 nM EC50 Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay F 9.46 pEC50 0.35 nM EC50 Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay F 9.68 pEC50 0.21 nM EC50 J Med Chem (2015) 58: 1992-2002 [PMID:25633969]
ChEMBL Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay F 9.72 pEC50 0.19 nM EC50 Eur J Med Chem (2019) 182: 111626-111626 [PMID:31445232]
ChEMBL Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay F 9.72 pEC50 0.19 nM EC50 Eur J Med Chem (2019) 182: 111626-111626 [PMID:31445232]
ChEMBL Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay F 9.74 pEC50 0.18 nM EC50 J Med Chem (2017) 60: 6273-6288 [PMID:28657744]
ChEMBL Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay F 9.77 pEC50 0.17 nM EC50 J Med Chem (2017) 60: 6273-6288 [PMID:28657744]
ChEMBL Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay F 9.77 pEC50 0.17 nM EC50 J Med Chem (2016) 59: 9866-9880 [PMID:27726356]
ChEMBL Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay F 9.78 pEC50 0.17 nM EC50 J Med Chem (2016) 59: 9866-9880 [PMID:27726356]
ChEMBL Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay F 9.85 pEC50 0.14 nM EC50 J Med Chem (2016) 59: 9866-9880 [PMID:27726356]
ChEMBL Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay F 9.87 pEC50 0.13 nM EC50 J Med Chem (2016) 59: 9866-9880 [PMID:27726356]
ChEMBL Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay F 10.05 pEC50 0.09 nM EC50 ACS Med Chem Lett (2011) 2: 929-932 [PMID:22778800]
ChEMBL Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay F 10.05 pEC50 0.09 nM EC50 J Med Chem (2009) 52: 1885-1902 [PMID:19284718]
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 7.5 pKd 7.5 - pKD J Med Chem (1993) 36: 1918-1919 [PMID:8515429]
ChEMBL The compound was tested for the binding affinity against 5-hydroxytryptamine 2C receptor using [3H]Mesulergine as radioligand. B 7.5 pKi 31.62 nM Ki J Med Chem (1999) 42: 4362-4379 [PMID:10543880]
ChEMBL Binding affinity was measured on 5-hydroxytryptamine 2C receptor in J1 cells transfected with rat 5-HT2C gene labeled with [3H]mesulergine B 7.64 pKi 23 nM Ki J Med Chem (1994) 37: 2828-2830 [PMID:8071931]
GtoPdb - - 7.9 pKi - - - Circulation (2000) 102: 2836-41 [PMID:11104741];
J Neurochem (1997) 69: 1138-44 [PMID:9282936]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 1C receptor was determined in male Sprague-Dawley rat brain. B 8 pKi 10 nM Ki J Med Chem (1990) 33: 755-758 [PMID:2299641]
ChEMBL Binding affinity against 5-hydroxytryptamine 1C receptor B 7.09 pIC50 81 nM IC50 J Med Chem (1992) 35: 4503-4505 [PMID:1447752]
ChEMBL Inhibition of radiolabeled [3H]mesulergine ligand binding to 5-hydroxytryptamine 2C receptor B 7.38 pIC50 42 nM IC50 J Med Chem (1997) 40: 3670-3678 [PMID:9357534]
ChEMBL Activity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cells F 8.55 pEC50 2.8 nM EC50 J Med Chem (2006) 49: 318-328 [PMID:16392816]
5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094132] [GtoPdb: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8]
ChEMBL Binding affinity for the 5-hydroxytryptamine 3 receptor was evaluated in vitro by examining its ability to displace [3H]-BRL 43694. B 6.84 pKi 144.54 nM Ki Bioorg Med Chem Lett (1993) 3: 205-208
ChEMBL Binding affinity towards 5-hydroxytryptamine 3 receptor B 6.92 pKi 120 nM Ki Bioorg Med Chem Lett (2002) 12: 2743-2747 [PMID:12217367]
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16]
ChEMBL The compound was tested for the binding affinity against 5-hydroxytryptamine 3 receptor using [3H]zacopride as radioligand. B 6.4 pKi 398.11 nM Ki J Med Chem (1999) 42: 4362-4379 [PMID:10543880]
ChEMBL The ability to inhibit [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor in rat brain cortices B 6.41 pKi 390 nM Ki J Med Chem (1992) 35: 1486-1489 [PMID:1573641]
ChEMBL Binding affinity was measured on 5-hydroxytryptamine 3 receptor in NG-108 cells labeled with [3H]GR-65630 B 6.49 pKi 320 nM Ki J Med Chem (1994) 37: 2828-2830 [PMID:8071931]
ChEMBL Ability to displace [3H]granisetron specifically bound to 5-hydroxytryptamine 3 receptor in rat cortical membrane B 6.92 pKi 120 nM Ki J Med Chem (1998) 41: 728-741 [PMID:9513601]
ChEMBL Inhibition of [3H]granisetron binding to 5-hydroxytryptamine 3 receptor of rat cortical membrane B 6.92 pKi 120 nM Ki J Med Chem (1999) 42: 1556-1575 [PMID:10229626]
ChEMBL Binding affinity at 5-hydroxytryptamine 3 receptor in rat entorhinal cortex by [3H]BRL-43694 displacement. B 7.06 pKi 87 nM Ki Bioorg Med Chem Lett (1996) 6: 263-266
ChEMBL Binding affinity for 5-hydroxytryptamine 3 receptor from rat cortex using [3H]BRL-43694 as radioligand B 7.18 pKi 66 nM Ki J Med Chem (1995) 38: 2692-2704 [PMID:7629808]
ChEMBL Inhibition of [3H]BRL-43694 binding to 5-hydroxytryptamine 3 receptor of rat cortical homogenate. B 6.14 pIC50 727 nM IC50 J Med Chem (1997) 40: 3670-3678 [PMID:9357534]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Antagonist activity at human 5HT3A receptor expressed in HEK293 cells by FMP assay F 6.3 pEC50 500 nM EC50 J Med Chem (2007) 50: 4616-4629 [PMID:17722904]
ChEMBL Antagonist activity at human 5HT3A receptor expressed in HEK293 cells by FMP assay F 6.34 pEC50 457.09 nM EC50 J Med Chem (2007) 50: 4616-4629 [PMID:17722904]
ChEMBL Partial agonist activity at human 5HT3A receptor expressed in HEK293 cells assessed as effect on serotonin-induced response F 6.75 pEC50 178 nM EC50 Bioorg Med Chem Lett (2011) 21: 58-61 [PMID:21146988]
ChEMBL Partial agonist activity at human 5HT3A receptor expressed in HEK293 cells assessed as decrease in 10 uM 5-chloroindole-induced increase in intracellular calcium release F 6.85 pEC50 141 nM EC50 Bioorg Med Chem Lett (2011) 21: 58-61 [PMID:21146988]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4972] [GtoPdb: 373] [UniProtKB: P23979]
ChEMBL Agonist activity at mouse 5HT3A I187A receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method F 4.05 pEC50 90000 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Selectivity ratio of EC50 for mouse 5HT3A Y143F receptor mutant to EC50 for wild type mouse 5HT3A receptor B 4.2 pEC50 63000 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Selectivity ratio of EC50 for mouse 5HT3A W183F receptor mutant to EC50 for wild type mouse 5HT3A receptor B 4.29 pEC50 51000 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Agonist activity at mouse 5HT3A Y153F receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method F 4.31 pEC50 49000 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Selectivity ratio of EC50 for mouse 5HT3A Y153A receptor mutant to EC50 for wild type mouse 5HT3A receptor B 4.38 pEC50 42000 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Agonist activity at mouse 5HT3A L184V receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method F 4.43 pEC50 37000 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Selectivity ratio of EC50 for mouse 5HT3A I187A receptor mutant to EC50 for wild type mouse 5HT3A receptor B 4.57 pEC50 27000 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Agonist activity at mouse 5HT3A T181A receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method F 4.62 pEC50 24000 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Agonist activity at mouse 5HT3A H185F receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method F 4.68 pEC50 20900 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Agonist activity at mouse 5HT3A H185Y receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method F 4.76 pEC50 17200 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Selectivity ratio of EC50 for mouse 5HT3A Y153F receptor mutant to EC50 for wild type mouse 5HT3A receptor B 4.82 pEC50 15000 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Selectivity ratio of EC50 for mouse 5HT3A L184V receptor mutant to EC50 for wild type mouse 5HT3A receptor B 4.96 pEC50 11000 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Agonist activity at mouse 5HT3A T186A receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method F 5.02 pEC50 9600 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Selectivity ratio of EC50 for mouse 5HT3A T181A receptor mutant to EC50 for wild type mouse 5HT3A receptor B 5.15 pEC50 7100 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Selectivity ratio of EC50 for mouse 5HT3A H185F receptor mutant to EC50 for wild type mouse 5HT3A receptor B 5.21 pEC50 6200 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Selectivity ratio of EC50 for mouse 5HT3A H185Y receptor mutant to EC50 for wild type mouse 5HT3A receptor B 5.29 pEC50 5100 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Agonist activity at mouse 5HT3A Q188A receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method F 5.36 pEC50 4400 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Agonist activity at mouse 5HT3A I190V receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method F 5.36 pEC50 4400 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Agonist activity at wild type mouse 5HT3A receptor expressed in Xenopus oocyte by two-electrode voltage patch clamp method F 5.47 pEC50 3400 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Agonist activity at mouse 5HT3A S182A receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method F 5.48 pEC50 3300 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Selectivity ratio of EC50 for mouse 5HT3A T186A receptor mutant to EC50 for wild type mouse 5HT3A receptor B 5.54 pEC50 2900 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Selectivity ratio of EC50 for mouse 5HT3A I190V receptor mutant to EC50 for wild type mouse 5HT3A receptor B 5.88 pEC50 1320 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Selectivity ratio of EC50 for mouse 5HT3A Q188A receptor mutant to EC50 for wild type mouse 5HT3A receptor B 5.89 pEC50 1300 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
ChEMBL Selectivity ratio of EC50 for mouse 5HT3A S182A receptor mutant to EC50 for wild type mouse 5HT3A receptor B 6.01 pEC50 980 nM EC50 Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2411] [GtoPdb: 373] [UniProtKB: P35563]
ChEMBL Response at rat 5-hydroxytryptamine 3a receptor expressed in xenopus oocytes F 4.92 pEC50 12000 nM EC50 Bioorg Med Chem Lett (2004) 14: 1849-1853 [PMID:15050614]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
GtoPdb - - 8.8 pKd - - - J Neurochem (2000) 74: 478-89 [PMID:10646498]
ChEMBL Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting B 5.98 pKi 1049 nM Ki J Med Chem (2009) 52: 2214-2225 [PMID:19334715]
ChEMBL Displacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cells B 6.3 pKi 500 nM Ki J Nat Prod (2006) 69: 1421-1424 [PMID:17067154]
ChEMBL Binding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assay B 6.61 pKi 246 nM Ki Eur J Med Chem (2019) 182: 111596-111596 [PMID:31419776]
ChEMBL Displacement of [3H]GR-113808 from human recombinant 5HT4b receptor expressed in HEK293 cells by scintillation counting B 6.96 pKi 109.65 nM Ki Eur J Med Chem (2009) 44: 2952-2959 [PMID:19223092]
GtoPdb - - 7 pKi - - - J Neurochem (1998) 70: 2252-61 [PMID:9603189];
Neuroreport (1997) 8: 3189-96 [PMID:9351641];
J Neurochem (1997) 69: 1810-9 [PMID:9349523];
J Neurochem (2000) 74: 478-89 [PMID:10646498];
Br J Pharmacol (2000) 129: 771-81 [PMID:10683202];
Br J Pharmacol (2000) 131: 827-35 [PMID:11030734];
Br J Pharmacol (2000) 130: 527-38 [PMID:10821780];
Br J Pharmacol (2004) 143: 549-60 [PMID:15466450];
Br J Pharmacol (2004) 143: 361-70 [PMID:15351779];
Naunyn Schmiedebergs Arch Pharmacol (2001) 363: 146-60 [PMID:11218067]
ChEMBL Displacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation counting B 7.53 pKi 29.51 nM Ki Eur J Med Chem (2009) 44: 2952-2959 [PMID:19223092]
ChEMBL Displacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assay B 6.49 pIC50 323 nM IC50 Eur J Med Chem (2019) 182: 111596-111596 [PMID:31419776]
ChEMBL Activity at SER4 receptor expressed in HEK293 cells assessed as increase in calcium by calcium imaging assay F 7 pEC50 100 nM EC50 Nature (2007) 450: 553-556 [PMID:18033297]
ChEMBL Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT F 7.92 pEC50 12 nM EC50 J Med Chem (2009) 52: 2214-2225 [PMID:19334715]
5-HT4 receptor in Mouse [GtoPdb: 9] [UniProtKB: P97288]
GtoPdb - - 7.2 pKi - - - FEBS Lett (1996) 398: 19-25 [PMID:8946946]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
GtoPdb - - 7.7 pKd - - - Eur J Pharmacol (1996) 304: 231-5 [PMID:8813606]
ChEMBL Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand B 6.73 pKi 187 nM Ki J Med Chem (1997) 40: 608-621 [PMID:9046352]
ChEMBL Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement. B 7.43 pKi 37.4 nM Ki Bioorg Med Chem Lett (1996) 6: 263-266
GtoPdb - - 8.2 pKi - - - EMBO J (1995) 14: 2806-15 [PMID:7796807];
Eur J Pharmacol (1996) 304: 231-5 [PMID:8813606];
Neuropharmacology (1997) 36: 671-9 [PMID:9225293]
ChEMBL Inhibition of radiolabeled [3H]GR-113808 ligand binding to 5-hydroxytryptamine 4 receptor B 6.83 pIC50 147 nM IC50 J Med Chem (1997) 40: 3670-3678 [PMID:9357534]
ChEMBL 5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae F 8.43 pIC50 3.7 nM IC50 Bioorg Med Chem Lett (1994) 4: 1433-1436
ChEMBL In vitro relaxation of carbachol pre-contracted rat oesophageal TMM. F 7.77 pEC50 17.1 nM EC50 Bioorg Med Chem Lett (1996) 6: 263-266
ChEMBL 5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae F 8.2 pEC50 6.31 nM EC50 Bioorg Med Chem Lett (1993) 3: 1375-1378
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
ChEMBL The compound was tested for their binding affinity towards 5-hydroxytryptamine 4 receptor from guinea pig striatum using [3H]GR-113808 as radioligand. B 6.64 pKi 230 nM Ki J Med Chem (1995) 38: 2692-2704 [PMID:7629808]
ChEMBL The compound was tested for the binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand. B 7 pKi 100 nM Ki J Med Chem (1999) 42: 4362-4379 [PMID:10543880]
ChEMBL Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum B 7 pKi 100 nM Ki J Med Chem (2009) 52: 3548-3562 [PMID:19425598]
ChEMBL Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum B 7 pKi 100 nM Ki J Med Chem (2009) 52: 6946-6950 [PMID:19831400]
ChEMBL Agonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contraction F 8 pEC50 10 nM EC50 Bioorg Med Chem Lett (2012) 22: 4849-4853 [PMID:22683222]
ChEMBL 5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum F 8.3 pEC50 5 nM EC50 J Med Chem (1997) 40: 608-621 [PMID:9046352]
ChEMBL 5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum F 8.3 pEC50 5 nM EC50 Bioorg Med Chem Lett (1994) 4: 1433-1436
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
ChEMBL Binding affinity for rodent 5-hydroxytryptamine 5A receptor B 6.6 pKi 250 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL Displacement of [3H]LSD from human 5HT5A receptor B 6.77 pKi 170 nM Ki J Med Chem (2011) 54: 5320-5334 [PMID:21726069]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting B 6.89 pKi 130 nM Ki J Med Chem (2017) 60: 349-361 [PMID:27997171]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand B 6.9 pKi 126 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
GtoPdb - - 6.9 pKi - - - FEBS Lett (1994) 355: 242-6 [PMID:7988681];
Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685]
ChEMBL Displacement of radiolabeled serotonin from human 5HT5A receptor B 6.96 pKi 110 nM Ki J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Binding affinity to human 5-HT5a receptor by radioligand displacement assay B 7.09 pKi 82 nM Ki Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL Binding affinity to human 5-HT5A receptor by radioligand displacement assay B 6.55 pIC50 280 nM IC50 Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting B 6.59 pIC50 260 nM IC50 J Med Chem (2017) 60: 349-361 [PMID:27997171]
ChEMBL Inhibition of human 5HT5A receptor B 6.74 pIC50 184 nM IC50 J Med Chem (2008) 51: 4150-4169 [PMID:18588282]
ChEMBL Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method B 6.74 pIC50 180 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL Displacement of radiolabeled serotonin from human 5HT5A receptor B 6.74 pIC50 180 nM IC50 J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cells B 6.74 pIC50 180 nM IC50 Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL Binding affinity to human 5-HT5a receptor by radioligand displacement assay B 6.8 pIC50 160 nM IC50 Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL Percent inhibition against 5-hydroxytryptamine 5A receptor at 1 uM B 7.1 pIC50 79 nM IC50 J Med Chem (2005) 48: 6887-6896 [PMID:16250647]
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3597] [GtoPdb: 10] [UniProtKB: P30966]
GtoPdb - - 6.6 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]
ChEMBL Binding affinity towards mouse 5-hydroxytryptamine 5A receptor B 6.82 pKi 150 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
5-HT5A receptor in Rat [GtoPdb: 10] [UniProtKB: P35364]
GtoPdb - - 6.6 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 6.9 pKi 125.89 nM Ki J Med Chem (2003) 46: 5117-5120 [PMID:14613313]
ChEMBL Binding affinity to 5-Ht6 receptor (unknown origin) B 7 pKi 100 nM Ki Bioorg Med Chem Lett (2016) 26: 2333-2338 [PMID:26996373]
ChEMBL Binding affinity against 5-hydroxytryptamine 6 receptor B 7 pKi 100 nM Ki Bioorg Med Chem Lett (2004) 14: 4569-4573 [PMID:15357994]
ChEMBL Displacement of radiolabeled serotonin from human 5HT6 receptor B 7.03 pKi 93 nM Ki J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Displacement of [3H]LSD from human 5HT6 receptor B 7.08 pKi 84 nM Ki J Med Chem (2011) 54: 5320-5334 [PMID:21726069]
ChEMBL Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand B 7.11 pKi 78 nM Ki Bioorg Med Chem Lett (2000) 10: 2295-2299 [PMID:11055342]
ChEMBL Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand B 7.12 pKi 75 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
ChEMBL Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand B 7.19 pKi 65 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting B 7.21 pKi 61 nM Ki J Med Chem (2017) 60: 349-361 [PMID:27997171]
ChEMBL Binding affinity to human 5-HT6 receptor by radioligand displacement assay B 7.3 pKi 50 nM Ki Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells B 7.48 pKi 33 nM Ki J Med Chem (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method B 7.48 pKi 33 nM Ki Eur J Med Chem (2015) 92: 221-235 [PMID:25557493]
GtoPdb - - 7.5 pKi - - - J Neurochem (1996) 66: 47-56 [PMID:8522988];
Mol Pharmacol (1998) 54: 577-583 [PMID:9730917];
Mol Pharmacol (1997) 52: 515-523 [PMID:9284367]
ChEMBL Inhibition of human 5HT6 receptor B 6.58 pIC50 262 nM IC50 J Med Chem (2008) 51: 4150-4169 [PMID:18588282]
ChEMBL Displacement of radiolabeled serotonin from human 5HT6 receptor B 6.7 pIC50 200 nM IC50 J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Binding affinity to human 5-HT6 receptor by radioligand displacement assay B 6.74 pIC50 180 nM IC50 Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting B 6.89 pIC50 130 nM IC50 J Med Chem (2017) 60: 349-361 [PMID:27997171]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells B 6.92 pIC50 120 nM IC50 Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting method B 6.92 pIC50 120 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL Binding affinity to human 5-HT6 receptor by radioligand displacement assay B 7 pIC50 100 nM IC50 Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [3H]LSD from human 5HT6 receptor by scintillation counting B 7.56 pIC50 27.5 nM IC50 J Med Chem (2010) 53: 2521-2527 [PMID:20170099]
ChEMBL Agonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay F 7.36 pEC50 43.6 nM EC50 J Med Chem (2018) 61: 10017-10039 [PMID:30383372]
ChEMBL Agonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay F 7.38 pEC50 42.1 nM EC50 Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805]
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 7.9 pKd - - - Neuropharmacology (1997) 36: 713-20 [PMID:9225298]
GtoPdb - - 7.9 pKi - - - Mol Pharmacol (1993) 43: 320-7 [PMID:7680751];
Neuropharmacology (1997) 36: 713-20 [PMID:9225298];
J Neurochem (1998) 71: 2169-77 [PMID:9798944];
Mol Pharmacol (1998) 54: 577-583 [PMID:9730917]
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 human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry B 8.4 pKd 3.98 nM Kd Eur J Med Chem (2014) 85: 716-726 [PMID:25128671]
ChEMBL Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor B 8.09 pKi 8.1 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells B 8.1 pKi 7.94 nM Ki Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003]
ChEMBL Displacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation counting B 8.22 pKi 6 nM Ki Eur J Med Chem (2016) 123: 180-190 [PMID:27475109]
ChEMBL Binding affinity of compound towards rodent 5-hydroxytryptamine 7 receptor B 8.4 pKi 4 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL Binding affinity against 5-hydroxytryptamine 7 human receptors B 8.5 pKi 3.16 nM Ki J Med Chem (2003) 46: 5117-5120 [PMID:14613313]
ChEMBL Displacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry B 8.67 pKi 2.12 nM Ki Bioorg Med Chem Lett (2016) 26: 4052-4056 [PMID:27396505]
ChEMBL Displacement of [3H]5-CT from human recombinant 5-HT7A receptor expressed in HEK cells by radioligand completion assay B 8.68 pKi 2.1 nM Ki J Med Chem (2021) 64: 13510-13523 [PMID:34467758]
ChEMBL Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis B 8.85 pKi 1.4 nM Ki Eur J Med Chem (2014) 80: 8-35 [PMID:24763360]
ChEMBL Displacement of [3H]LSD from human 5-HT7 receptor expressed in CHO cells B 9.1 pKi 0.8 nM Ki Eur J Med Chem (2015) 92: 221-235 [PMID:25557493]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cells B 9.1 pKi 0.8 nM Ki J Med Chem (2014) 57: 4543-4557 [PMID:24805037]
GtoPdb - - 9.6 pKi - - - Biochem Pharmacol (2003) 65: 435-40 [PMID:12527336];
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 Displacement of radiolabeled serotonin from human 5HT7 receptor B 9.66 pKi 0.22 nM Ki J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cells after 120 mins by scintillation counting B 9.77 pKi 0.17 nM Ki J Med Chem (2017) 60: 349-361 [PMID:27997171]
ChEMBL Displacement of [3H]LSD from human 5HT7 receptor B 9.89 pKi 0.13 nM Ki J Med Chem (2011) 54: 5320-5334 [PMID:21726069]
ChEMBL Binding affinity to human 5-HT7 receptor by radioligand displacement assay B 9.96 pKi 0.11 nM Ki Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells B 8.59 pIC50 2.55 nM IC50 J Nat Prod (2003) 66: 535-537 [PMID:12713409]
ChEMBL Inhibition of human 5HT7 receptor B 8.82 pIC50 1.5 nM IC50 J Med Chem (2008) 51: 4150-4169 [PMID:18588282]
ChEMBL Displacement of radiolabeled serotonin from human 5HT7 receptor B 9.21 pIC50 0.61 nM IC50 J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Binding affinity to human 5-HT7 receptor by radioligand displacement assay B 9.31 pIC50 0.49 nM IC50 Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cells after 120 mins by scintillation counting B 9.33 pIC50 0.47 nM IC50 J Med Chem (2017) 60: 349-361 [PMID:27997171]
ChEMBL Binding affinity to human 5-HT7 receptor by radioligand displacement assay B 9.54 pIC50 0.29 nM IC50 Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cells B 9.6 pIC50 0.25 nM IC50 Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells measured after 120 mins by scintillation counting method B 9.6 pIC50 0.25 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay F 6.95 pEC50 112.2 nM EC50 J Med Chem (2021) 64: 7453-7467 [PMID:34032427]
ChEMBL Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay F 6.96 pEC50 110 nM EC50 J Med Chem (2021) 64: 7453-7467 [PMID:34032427]
ChEMBL Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis F 7.15 pEC50 70 nM EC50 Bioorg Med Chem (2020) 28: 115578-115578 [PMID:32631561]
ChEMBL Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay F 7.32 pEC50 48 nM EC50 J Med Chem (2018) 61: 7218-7233 [PMID:30028132]
ChEMBL Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay F 7.32 pEC50 47.86 nM EC50 J Med Chem (2018) 61: 7218-7233 [PMID:30028132]
ChEMBL Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay F 7.77 pEC50 17 nM EC50 J Med Chem (2014) 57: 6879-6884 [PMID:25073094]
ChEMBL Agonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assay F 7.82 pEC50 15 nM EC50 J Med Chem (2009) 52: 2384-2392 [PMID:19326916]
ChEMBL Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis F 8.03 pEC50 9.33 nM EC50 J Med Chem (2021) 64: 7453-7467 [PMID:34032427]
ChEMBL Agonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as increase in serotonin-induced cAMP level after 1 hr by TR-FRET assay F 8.15 pEC50 7 nM EC50 Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027]
ChEMBL Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay F 8.24 pEC50 5.8 nM EC50 Eur J Med Chem (2016) 123: 180-190 [PMID:27475109]
ChEMBL Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay F 8.24 pEC50 5.75 nM EC50 Eur J Med Chem (2016) 123: 180-190 [PMID:27475109]
ChEMBL Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assay B 8.24 pEC50 5.7 nM EC50 Bioorg Med Chem (2019) 27: 4163-4173 [PMID:31383628]
ChEMBL Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assay B 8.27 pEC50 5.37 nM EC50 Bioorg Med Chem (2019) 27: 4163-4173 [PMID:31383628]
ChEMBL Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis F 8.35 pEC50 4.5 nM EC50 J Med Chem (2021) 64: 7453-7467 [PMID:34032427]
ChEMBL Agonist activity at human 5-HT7A receptor expressed in HEK cell membranes incubated for 20 mins by cAMP functional assay F 8.44 pEC50 3.66 nM EC50 Eur J Med Chem (2021) 214: 113243-113243 [PMID:33582388]
5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
GtoPdb - - 8.3 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 Binding affinity towards rat 5-hydroxytryptamine 7 receptor B 8 pKi 10 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells at 10 uM B 8.13 pKi 7.33 nM Ki Bioorg Med Chem (2007) 15: 5316-5321 [PMID:17517509]
GtoPdb - - 9.2 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 9.22 pKi 0.6 nM Ki J Med Chem (2003) 46: 5365-5374 [PMID:14640545]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL Ability to displace [3H]paroxetine bound to Serotonin transporter receptor in rat forebrain B 6.13 pKi 740 nM Ki J Med Chem (1998) 41: 728-741 [PMID:9513601]
ChEMBL Binding affinity towards Serotonin transporter was determined in rat forebrain membrane B 6.13 pKi 740 nM Ki J Med Chem (1999) 42: 1556-1575 [PMID:10229626]
Organic cation transporter 3/Solute carrier family 22 member 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770033] [GtoPdb: 1021] [UniProtKB: O88446]
ChEMBL TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in OCT3-expressing HRPE cells F 4.01 pIC50 97000 nM IC50 J Biol Chem (1998) 273: 32776-32786 [PMID:9830022]
Vesicular monoamine transporter 2/Synaptic vesicular amine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1893] [GtoPdb: 1012] [UniProtKB: Q05940]
ChEMBL Displacement of [3H]reserpine from human VMAT2 expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method B 5.11 pKi 7690 nM Ki J Med Chem (2018) 61: 9121-9131 [PMID:30240563]
ChEMBL Displacement of [3H](+)-syn-Ethyl 1-(2-(2,4-Dioxo-1,2-dihydroquinazolin-3(4H)-yl)ethyl)-4-(4-fluorophenyl)piperidine-3-carboxylate from human VMAT2 expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method B 5.64 pKi 2290 nM Ki J Med Chem (2018) 61: 9121-9131 [PMID:30240563]
ChEMBL Inhibition of human VMAT2 expressed in HEK293 cell membranes assessed as reduction in [3H[-5HT uptake pre-incubated for 10 mins before [3H[-5HT addition and measured after 6 mins B 5.84 pIC50 1430 nM IC50 J Med Chem (2018) 61: 9121-9131 [PMID:30240563]
Vesicular monoamine transporter 2/Synaptic vesicular amine transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295886] [GtoPdb: 1012] [UniProtKB: Q8BRU6]
ChEMBL Inhibition of VMAT2 in C57Bl/6J mouse striatal membranes assessed as reduction in [3H[-5HT uptake pre-incubated for 10 mins before [3H[-5HT addition and measured after 8 mins B 7.01 pIC50 98 nM IC50 J Med Chem (2018) 61: 9121-9131 [PMID:30240563]
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 4.45 pEC50 35100 nM EC50 ACS Med Chem Lett (2022) 13: 92-98 [PMID:35047111]
D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
GtoPdb - - 5.5 pKi - - - Nature (1991) 350: 614-9 [PMID:1826762]
5-HT3AB in Human [GtoPdb: 378]
GtoPdb - - 6 pKi - - - Neuropharmacology (2001) 41: 282-4 [PMID:11489465]
GtoPdb - - 5.8 pEC50 - - - Nature (1999) 397: 359-63 [PMID:9950429];
J Biol Chem (1999) 274: 30799-810 [PMID:10521471];
J Pharmacol Exp Ther (2005) 315: 771-6 [PMID:16081679];
Mol Pharmacol (2000) 57: 1114-22 [PMID:10825381]
5-HT3A in Human [GtoPdb: 379]
GtoPdb - - 6.9 pKi - - - Mol Pharmacol (1998) 53: 202-12 [PMID:9463477];
Neuropharmacology (2001) 41: 282-4 [PMID:11489465];
Br J Pharmacol (1996) 118: 1237-45 [PMID:8818349];
Eur J Pharmacol (2000) 409: 195-201 [PMID:11104834]
GtoPdb - - 6.4 pEC50 - - - Mol Pharmacol (1995) 48: 1054-62 [PMID:8848005];
Mol Pharmacol (2000) 57: 1114-22 [PMID:10825381];
Nature (1999) 397: 359-63 [PMID:9950429];
J Biol Chem (1999) 274: 30799-810 [PMID:10521471];
Mol Pharmacol (1998) 53: 202-12 [PMID:9463477];
Mol Pharmacol (1995) 48: 407-16 [PMID:7565620];
J Pharmacol Exp Ther (2005) 315: 771-6 [PMID:16081679]
Proton-coupled Amino acid Transporter 1 in Human [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
GtoPdb - - 2.2 pKi 5700000 nM Ki FASEB J (2005) 19: 1468-73 [PMID:16126914]

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]