yohimbine [Ligand Id: 102] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL15245 (Yohimbine)
  • 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]
  • 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]
  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • Dual specificity phosphatase Cdc25A in Human [ChEMBL: CHEMBL3775] [UniProtKB: P30304]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 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 in Rat [GtoPdb: 7] [UniProtKB: P30994]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Mouse [ChEMBL: CHEMBL3006] [GtoPdb: 8] [UniProtKB: P34968]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
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  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor in Mouse [GtoPdb: 2] [UniProtKB: P28334]
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  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
  • 5-HT1F receptor in Rat [GtoPdb: 5] [UniProtKB: P30940]
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  • 5-HT5A receptor in Human [GtoPdb: 10] [UniProtKB: P47898]
  • 5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966]
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  • 5-HT7 receptor in Human [GtoPdb: 12] [UniProtKB: P34969]
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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 Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor B 6.4 pKd 398.11 nM Kd J. Med. Chem. (1984) 27: 495-503 [PMID:6142954]
ChEMBL Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells B 5.98 pKi 1057 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand B 6.66 pKi 220 nM Ki J. Med. Chem. (1983) 26: 1696-1701 [PMID:6139479]
ChEMBL Evaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortex B 6.66 pKi 220 nM Ki J. Med. Chem. (1985) 28: 1756-1759 [PMID:2999400]
ChEMBL Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor B 6.7 pKi 200 nM Ki J. Med. Chem. (1984) 27: 1182-1185 [PMID:6088770]
ChEMBL Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pineal B 8.44 pKi 3.6 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
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 6.3 pKi 500 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 5.91 pIC50 1235 nM IC50 DrugMatrix in vitro pharmacology data
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Inhibition of [3H]prazosin binding to human Alpha-1B adrenergic receptor expressed in CHO cells B 6.02 pKi 966 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL Binding affinity against Alpha-1B adrenergic receptor from human clone B 8.14 pKi 7.2 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Binding affinity against Alpha-1B adrenergic receptor from hamster clones. B 8.96 pKi 1.1 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
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 6.18 pKi 658 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 5.93 pIC50 1188 nM IC50 DrugMatrix in vitro pharmacology data
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 6.3 pKi 498 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of [3H]prazosin binding to human Alpha-1D adrenergic receptor expressed in CHO cells B 6.54 pKi 289 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL Binding affinity against Alpha-1D adrenergic receptor, from human clones. B 8.8 pKi 1.6 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 5.99 pIC50 1013 nM IC50 DrugMatrix in vitro pharmacology data
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
ChEMBL Binding affinity against Alpha-1D adrenergic receptor, from rat clones. B 7.28 pKi 52 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor B 8.12 pKi 7.5 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 mins B 8.5 pKi 3.13 nM Ki J Med Chem (2020) 63: 433-439 [PMID:31834797]
ChEMBL Displacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 mins B 8.51 pKi 3.1 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Inhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptor B 8.51 pKi 3.1 nM Ki J. Med. Chem. (1999) 42: 5181-5187 [PMID:10602703]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 8.64 pKi 2.31 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL In vitro binding affinity towards alpha-2a adrenergic receptor B 8.85 pKi 1.4 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 2758-2760 [PMID:15911252]
GtoPdb - - 9.2 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470];
Mol Pharmacol (1992) 42: 1-5 [PMID:1353247];
Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642]
ChEMBL Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand B 9.38 pKi 0.42 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 627-630 [PMID:10762040]
ChEMBL Displacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 mins B 8.08 pIC50 8.4 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 8.21 pIC50 6.15 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]MK912 from human recombinant adrenergic alpha2A receptor expressed in Sf9 cells B 8.07 pEC50 8.5 nM EC50 J. Nat. Prod. (2006) 69: 432-435 [PMID:16562853]
Alpha-2a adrenergic receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2350] [UniProtKB: P18871]
ChEMBL Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-clone B 8.36 pKi 4.4 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 Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand B 7.31 pKi 49 nM Ki J. Med. Chem. (1983) 26: 1696-1701 [PMID:6139479]
ChEMBL Evaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortex B 7.31 pKi 49 nM Ki J. Med. Chem. (1985) 28: 1756-1759 [PMID:2999400]
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL Displacement of [125I]Clonidine from adrenergic alpha2B receptor (unknown origin) B 7.54 pKi 28.84 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 576-579 [PMID:24365159]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 8.1 pKi 7.95 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL In vitro binding affinity towards alpha-2b adrenergic receptor B 8.15 pKi 7.1 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 2758-2760 [PMID:15911252]
ChEMBL Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2B adrenergic receptor B 8.34 pKi 4.6 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL Displacement of [125I]Clonidine from adrenergic alpha2B receptor (unknown origin) B 8.49 pKi 3.2 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 576-579 [PMID:24365159]
ChEMBL Binding affinity against human alpha 2b-adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand B 8.7 pKi 2.01 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 627-630 [PMID:10762040]
GtoPdb - - 8.9 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470];
Mol Pharmacol (1992) 42: 1-5 [PMID:1353247];
Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642]
ChEMBL Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2B receptor expressed in CHO cell membranes incubated for 60 mins B 8.94 pKi 1.16 nM Ki J Med Chem (2020) 63: 433-439 [PMID:31834797]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 7.77 pIC50 17 nM IC50 DrugMatrix in vitro pharmacology data
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
ChEMBL Inhibition of [3H]- Yohimbine binding against rat kidney cortex Alpha-2B adrenergic receptor B 8.7 pKi 2 nM Ki J. Med. Chem. (1999) 42: 5181-5187 [PMID:10602703]
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 8.29 pKi 5.16 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptor B 8.64 pKi 2.3 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine B 9.06 pKi 0.88 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 2758-2760 [PMID:15911252]
ChEMBL Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C receptor expressed in CHO cell membranes incubated for 60 mins B 9.1 pKi 0.8 nM Ki J Med Chem (2020) 63: 433-439 [PMID:31834797]
ChEMBL Displacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cells B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL Displacement of [3H]RX-821002 from human adrenergic alpha2C receptor expressed in CHO cells B 9.3 pKi 0.5 nM Ki Eur. J. Med. Chem. (2015) 92: 221-235 [PMID:25557493]
GtoPdb - - 9.5 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470];
Mol Pharmacol (1992) 42: 1-5 [PMID:1353247];
Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 7.44 pIC50 36 nM IC50 DrugMatrix in vitro pharmacology data
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 5.69 pIC50 2031.7 nM IC50 DrugMatrix in vitro pharmacology data
DNA topoisomerase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781] [GtoPdb: 2636] [UniProtKB: P11387]
ChEMBL Inhibition of human recombinant DNA topoisomerase1 B 4.52 pIC50 30000 nM IC50 J. Nat. Prod. (2005) 68: 848-852 [PMID:15974606]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 6.16 pKi 687 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 5.69 pIC50 2060 nM IC50 DrugMatrix in vitro pharmacology data
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL In vitro inhibition of specific binding of [3H]-YM 09151-2 to Dopamine receptor D2 site in rat striatal tissue. B 5.95 pIC50 1125 nM IC50 J. Med. Chem. (2000) 43: 3653-3664 [PMID:11020279]
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 5.61 pKi 2430 nM Ki J. Med. Chem. (1993) 36: 1499-1500 [PMID:8098771]
Dual specificity phosphatase Cdc25A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3775] [UniProtKB: P30304]
ChEMBL Inhibition of His-tagged Cdc25A expressed in the Escherichia coli BL21(DE3) using p-nitrophenyl phosphate as substrate for 80 mins by spectrophotometry B 4.65 pIC50 22300 nM IC50 J. Med. Chem. (2012) 55: 5989-6001 [PMID:22537178]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL Inhibitory activity against norepinephrine (NE) uptake in rat whole brain synaptosome preparation F 4.7 pIC50 >20000 nM IC50 J. Med. Chem. (1996) 39: 570-581 [PMID:8558529]
5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb - - 7.3 pKi - - - Synapse (2000) 35: 79-95 [PMID:10611634]
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 7.14 pKi 72 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 6.9 pIC50 126 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Binding affinity for 5-HT 2A in rat stomach fundus B 5.79 pKi 1621.81 nM Ki J. Med. Chem. (1996) 39: 2773-2780 [PMID:8709108]
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 7.33 pKi 47 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 7.9