oxymetazoline [Ligand Id: 124] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL762 (Nasacon, Ocuclear, Operil, Oxymetazoline)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
  • Alpha-1b adrenergic receptor in Hamster [ChEMBL: CHEMBL3122] [UniProtKB: P18841]
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
  • Alpha-2a adrenergic receptor in Pig [ChEMBL: CHEMBL2350] [UniProtKB: P18871]
  • Alpha-2a adrenergic receptor in Bovine [ChEMBL: CHEMBL4744] [UniProtKB: Q28838]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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  • 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/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]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes B 7.8 pKi 15.85 nM Ki J Med Chem (2002) 45: 2229-2239 [PMID:12014961]
GtoPdb - - 8.2 pKi - - - Br J Pharmacol (2017) 174: 2318-2333 [PMID:28444738];
Mol Pharmacol (2011) 79: 298-307 [PMID:20978120];
Br J Pharmacol (1995) 116: 1611-8 [PMID:8564227];
Eur J Pharmacol (1995) 291: 327-34 [PMID:8719417];
Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529];
J Pharmacol Exp Ther (1995) 272: 134-42 [PMID:7815325];
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358];
Br J Pharmacol (1999) 127: 962-8 [PMID:10433504]
ChEMBL In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate F 6.46 pEC50 346.74 nM EC50 J Med Chem (1996) 39: 4116-4119 [PMID:8831777]
ChEMBL Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor F 7.69 pEC50 20.42 nM EC50 J Med Chem (2002) 45: 2229-2239 [PMID:12014961]
ChEMBL Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts. F 7.7 pEC50 19.95 nM EC50 Bioorg Med Chem Lett (2001) 11: 2871-2874 [PMID:11597419]
ChEMBL In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay F 7.7 pEC50 19.95 nM EC50 Bioorg Med Chem Lett (2002) 12: 575-579 [PMID:11844675]
GtoPdb - - 9.3 pEC50 - - - Mol Pharmacol (2011) 79: 298-307 [PMID:20978120];
Br J Pharmacol (2017) 174: 2318-2333 [PMID:28444738];
Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Binding affinity towards bovine clonal Alpha-1A adrenergic receptor B 7.88 pKi 13.18 nM Ki J Med Chem (1996) 39: 4116-4119 [PMID:8831777]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 7.8 pKi 16 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands B 8.19 pKi 6.46 nM Ki J Med Chem (1996) 39: 4116-4119 [PMID:8831777]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 7.42 pIC50 38 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens F 6.54 pEC50 288.4 nM EC50 J Med Chem (1996) 39: 4116-4119 [PMID:8831777]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Affinity to human Alpha-1B adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes B 6.08 pKi 831.76 nM Ki J Med Chem (2002) 45: 2229-2239 [PMID:12014961]
GtoPdb - - 6.5 pKi - - - Mol Pharmacol (1995) 48: 250-8 [PMID:7651358];
Eur J Pharmacol (1995) 291: 327-34 [PMID:8719417];
Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529]
ChEMBL Agonist potency at Alpha-1B adrenergic receptor expressed in rat-1 fibroblasts F 4.6 pEC50 <25118.86 nM EC50 J Med Chem (2002) 45: 2229-2239 [PMID:12014961]
ChEMBL Potency against cloned human alpha 1B adrenoceptor expressed in rat-1 fibroblasts. F 5.3 pEC50 <5011.87 nM EC50 Bioorg Med Chem Lett (2001) 11: 2871-2874 [PMID:11597419]
ChEMBL In vitro activation of human Alpha-1B receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay F 5.3 pEC50 <5011.87 nM EC50 Bioorg Med Chem Lett (2002) 12: 575-579 [PMID:11844675]
GtoPdb - - 7.4 pEC50 - - - Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529]
Alpha-1b adrenergic receptor in Hamster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3122] [UniProtKB: P18841]
ChEMBL Binding affinity towards hamster clonal Alpha-1B adrenergic receptor B 6.69 pKi 204.17 nM Ki J Med Chem (1996) 39: 4116-4119 [PMID:8831777]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 6.16 pKi 689 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 5.9 pIC50 1245 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL In vitro agonist potency towards Alpha-1B adrenergic receptor in rat spleen F 6.47 pEC50 338.84 nM EC50 J Med Chem (1996) 39: 4116-4119 [PMID:8831777]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 5.85 pKi 1398 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Affinity to human Alpha-1D adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes B 5.87 pKi 1348.96 nM Ki J Med Chem (2002) 45: 2229-2239 [PMID:12014961]
GtoPdb - - 6.4 pKi - - - Mol Pharmacol (1995) 48: 250-8 [PMID:7651358];
Eur J Pharmacol (1995) 291: 327-34 [PMID:8719417];
Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 5.55 pIC50 2844 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Agonist potency at Alpha-1D adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1D adrenergic receptor F 4.6 pEC50 <25118.86 nM EC50 J Med Chem (2002) 45: 2229-2239 [PMID:12014961]
ChEMBL Potency against cloned human alpha 1D-adrenoceptor expressed in rat-1 fibroblasts. F 5.3 pEC50 <5011.87 nM EC50 Bioorg Med Chem Lett (2001) 11: 2871-2874 [PMID:11597419]
ChEMBL In vitro activation of human alpha-1D receptor expressed in rat-1 fibroblasts via calcium using mobilization through the Gq coupled PLC pathway as functional assay F 5.3 pEC50 <5011.87 nM EC50 Bioorg Med Chem Lett (2002) 12: 575-579 [PMID:11844675]
GtoPdb - - 7.3 pEC50 - - - Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
GtoPdb - - 6.2 pKi - - - Mol Pharmacol (1994) 46: 929-36 [PMID:7969082]
ChEMBL Binding affinity towards rat clonal Alpha-1D adrenergic receptor B 6.48 pKi 331.13 nM Ki J Med Chem (1996) 39: 4116-4119 [PMID:8831777]
ChEMBL In vitro agonist potency towards Alpha-1D adrenergic receptor in rat aorta F 5.08 pEC50 8317.64 nM EC50 J Med Chem (1996) 39: 4116-4119 [PMID:8831777]
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells B 7.79 pKi 16.22 nM Ki J Med Chem (2002) 45: 2229-2239 [PMID:12014961]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 8.06 pKi 8.64 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 8.6 pKi - - - Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427];
J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470];
Trends Pharmacol Sci (1997) 18: 211-9 [PMID:9227000];
Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
ChEMBL Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin) B 8.64 pKi 2.29 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin) B 9.54 pKi 0.29 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 7.64 pIC50 23 nM IC50 DrugMatrix in vitro pharmacology data
GtoPdb inhibition of forskolin stimulated cAMP generation - 8.4 pIC50 - - - Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
ChEMBL Agonist potency at Alpha-2A stably expressed in CHO cells. F 8.48 pEC50 3.31 nM EC50 J Med Chem (2002) 45: 2229-2239 [PMID:12014961]
Alpha-2a adrenergic receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2350] [UniProtKB: P18871]
ChEMBL Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-clone B 7.68 pKi 21 nM Ki J Med Chem (1995) 38: 3415-3444 [PMID:7658428]
Alpha-2a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4744] [UniProtKB: Q28838]
ChEMBL Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal B 8.82 pKi 1.5 nM Ki J Med Chem (1995) 38: 3415-3444 [PMID:7658428]
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL Affinity to human Alpha-2B adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells B 5.27 pKi 5370.32 nM Ki J Med Chem (2002) 45: 2229-2239 [PMID:12014961]
GtoPdb - - 6.2 pKi - - - Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427];
J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470];
Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 6.24 pKi 581 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 5.9 pIC50 1273 nM IC50 DrugMatrix in vitro pharmacology data
GtoPdb inhibition of forskolin stimulated cAMP generation - 8.8 pIC50 - - - Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
GtoPdb cAMP generation - 7.7 pEC50 - - - Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 6.42 pKi 383 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 6.7 pKi - - - Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427];
J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470];
Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495];
Brain Res Bull (2014) 107: 89-101 [PMID:25080296]
ChEMBL Affinity to human Alpha-2C adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells B 7.23 pKi 58.88 nM Ki J Med Chem (2002) 45: 2229-2239 [PMID:12014961]
ChEMBL Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin) B 8.3 pKi 5.01 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin) B 9 pKi 1 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 5.58 pIC50 2633 nM IC50 DrugMatrix in vitro pharmacology data
GtoPdb inhibition of cAMP production - 8.2 pIC50 - - - Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495];
Brain Res Bull (2014) 107: 89-101 [PMID:25080296]
GtoPdb β-arrestin recruitment and internalization - 6.92 pEC50 - - - Brain Res Bull (2014) 107: 89-101 [PMID:25080296]
CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635]
ChEMBL DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 6.7 pIC50 200 nM IC50 DrugMatrix in vitro pharmacology data
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.34 pKi 455 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.49 pIC50 3261 nM IC50 DrugMatrix in vitro pharmacology data
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.02 pKi 957 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.88 pIC50 1332 nM IC50 DrugMatrix in vitro pharmacology data
Nischarin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3923] [UniProtKB: Q9Y2I1]
ChEMBL Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR B 8.21 pKi 6.2 nM Ki Bioorg Med Chem (2008) 16: 7134-7140 [PMID:18621536]
ChEMBL Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR B 8.21 pKi 6.19 nM Ki Bioorg Med Chem (2008) 16: 7134-7140 [PMID:18621536]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 8.49 pKi 3.21 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 8.25 pIC50 5.61 nM IC50 DrugMatrix in vitro pharmacology data
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 9.5 pKi - - - J Med Chem (1998) 41: 2243-51 [PMID:9632357]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand B 9.52 pKi 0.3 nM Ki J Med Chem (1998) 41: 2243-2251 [PMID:9632357]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) B 9.04 pKi 0.91 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) B 8.7 pIC50 2 nM IC50 DrugMatrix in vitro pharmacology data
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 1D receptor using [3H]5-HT trifluoroacetate as radioligand B 9.4 pKi 0.4 nM Ki J Med Chem (1998) 41: 2243-2251 [PMID:9632357]
GtoPdb - - 9.4 pKi - - - J Med Chem (1998) 41: 2243-51 [PMID:9632357]
ChEMBL Compound was tested for 5-hydroxytryptamine 1D like receptor-mediated vascular effect in rabbit saphenous vein (RSV) F 6.86 pEC50 137 nM EC50 J Med Chem (1998) 41: 2243-2251 [PMID:9632357]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 6.44 pKi 367 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 5.89 pIC50 1285 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.71 pKi 1945 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.51 pIC50 3056 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 6.52 pKi 303 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 6.8 pKi - - - J Neurochem (1999) 72: 2127-34 [PMID:10217294]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 6.24 pIC50 578 nM IC50 DrugMatrix in vitro pharmacology data
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.11 pKi 775 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.78 pIC50 1670 nM IC50 DrugMatrix in vitro pharmacology data

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]