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

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ChEMBL ligand: CHEMBL762 (Nasacon, Ocuclear, Operil, Oximetazolina, 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 - - - Mol Pharmacol (1995) 48: 250-8 [PMID:7651358];
Eur J Pharmacol (1995) 291: 327-34 [PMID:8719417];
Br J Pharmacol (1999) 127: 962-8 [PMID:10433504];
J Pharmacol Exp Ther (1995) 272: 134-42 [PMID:7815325];
Mol Pharmacol (2011) 79: 298-307 [PMID:20978120];
Br J Pharmacol (1995) 116: 1611-8 [PMID:8564227];
Br J Pharmacol (2017) 174: 2318-2333 [PMID:28444738];
Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529]
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 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]