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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  • microtubule affinity regulating kinase 4/MAP/microtubule affinity-regulating kinase 4 in Human [ChEMBL: CHEMBL5754] [GtoPdb: 2100] [UniProtKB: Q96L34]
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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]
microtubule affinity regulating kinase 4/MAP/microtubule affinity-regulating kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5754] [GtoPdb: 2100] [UniProtKB: Q96L34]
ChEMBL Inhibition of MARK4 (unknown origin) ATPase activity using ATP as substrate incubated for 1.5 hr in presence of MgCl2 by Biomol green reagent based ELISA B 5.52 pIC50 2990 nM IC50 RSC Med Chem (2022) 13: 737-745 [PMID:35814926]
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 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assay F 6.4 pEC50 398.11 nM EC50 Eur J Med Chem (2022) 233: 114218-114218 [PMID:35248836]
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 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 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 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 Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 40 mins by TR-FRET assay F 7.96 pEC50 10.96 nM EC50 Eur J Med Chem (2022) 233: 114218-114218 [PMID:35248836]
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 Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as stimulation of ERK1/2 phosphorylation incubated for 15 mins by Alpha LISA assay F 8 pEC50 10 nM EC50 Eur J Med Chem (2022) 233: 114218-114218 [PMID:35248836]
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 - - - 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];
Eur J Pharmacol (1996) 314: 365-72 [PMID:8957260];
Mol Pharmacol (1996) 50: 1567-80 [PMID:8967979];
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 Agonist activity at human 5HT2A S159A mutant transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay B 5.78 pEC50 1672 nM EC50 J Med Chem (2022) 65: 12031-12043 [PMID:36099411]
ChEMBL Agonist activity at human 5HT2A S159A mutant transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay B 6.18 pEC50 661 nM EC50 J Med Chem (2022) 65: 12031-12043 [PMID:36099411]
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 transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay F 6.89 pEC50 130 nM EC50 J Med Chem (2022) 65: 12031-12043 [PMID:36099411]
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 Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay F 7.92 pEC50 12.1 nM EC50 J Med Chem (2022) 65: 12031-12043 [PMID:36099411]
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 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 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 5-HT2AR (unknown origin) stably expressed in HEK293 cells measured after 1 hr by fluorescence based Ca2+/Fluo-4 assay B 8.52 pEC50 3 nM EC50 ACS Med Chem Lett (2023) 14: 319-325 [PMID:36923922]
ChEMBL Agonist activity at 5-HT2AR (unknown origin) stably expressed in HEK293 cells measured after 1 hr by fluorescence based Ca2+/Fluo-4 assay B 8.53 pEC50 2.95 nM EC50 ACS Med Chem Lett (2023) 14: 319-325 [PMID:36923922]
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 5-HT2CR (unknown origin) stably expressed in HEK293 cells measured after 1 hr by fluorescence based Ca2+/Fluo-4 assay B 8.92 pEC50 1.2 nM EC50 ACS Med Chem Lett (2023) 14: 319-325 [PMID:36923922]
ChEMBL Agonist activity at 5-HT2CR (unknown origin) stably expressed in HEK293 cells measured after 1 hr by fluorescence based Ca2+/Fluo-4 assay B 8.92 pEC50 1.2 nM EC50 ACS Med Chem Lett (2023) 14: 319-325 [PMID:36923922]
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 by FLIPR assay F 10.05 pEC50 0.09 nM EC50 J Med Chem (2009) 52: 1885-1902 [PMID:19284718]
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]
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 - - - Nature (1999) 397: 359-63 [PMID:9950429];
Mol Pharmacol (1995) 48: 1054-62 [PMID:8848005];
Mol Pharmacol (1995) 48: 407-16 [PMID:7565620];
J Biol Chem (1999) 274: 30799-810 [PMID:10521471];
Mol Pharmacol (1998) 53: 202-12 [PMID:9463477];
J Pharmacol Exp Ther (2005) 315: 771-6 [PMID:16081679];
Mol Pharmacol (2000) 57: 1114-22 [PMID:10825381]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]