prazosin [Ligand Id: 503] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2 (Prazosin, CP-12299, CP-122991)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
  • Alpha-1a adrenergic receptor in Rabbit [ChEMBL: CHEMBL3637] [UniProtKB: O02824]
  • 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]
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909]
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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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  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
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  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • MMP1/Matrix metalloproteinase-1 in Human [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956]
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  • MMP9/Matrix metalloproteinase 9 in Human [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780]
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  • Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8]
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  • MATE2/Multidrug and toxin extrusion protein 2 in Human [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8]
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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 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]
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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 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]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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  • Organic cation transporter 2/Solute carrier family 22 member 2 in Human [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
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  • Organic cation transporter 3/Solute carrier family 22 member 3 in Human [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751]
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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 Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin) B 8.73 pKi 1.86 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 576-579 [PMID:24365159]
ChEMBL Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand B 9.21 pKi 0.61 nM Ki J. Med. Chem. (2001) 44: 2403-2410 [PMID:11448222]
ChEMBL In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes B 9.22 pKi 0.6 nM Ki J. Med. Chem. (1999) 42: 4778-4793 [PMID:10579841]
ChEMBL Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin) B 9.23 pKi 0.59 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins B 9.23 pKi 0.59 nM Ki Eur J Med Chem (2017) 136: 259-269 [PMID:28499171]
ChEMBL Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement. B 9.23 pKi 0.59 nM Ki J. Med. Chem. (1998) 41: 4844-4853 [PMID:9822553]
ChEMBL Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi B 9.23 pKi 0.59 nM Ki J. Med. Chem. (2003) 46: 4895-4903 [PMID:14584940]
ChEMBL Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cells B 9.23 pKi 0.59 nM Ki J. Med. Chem. (2005) 48: 28-31 [PMID:15633998]
ChEMBL Binding affinity to adrenergic alpha1A receptor (unknown origin) B 9.23 pKi 0.59 nM Ki Med Chem Res (2011) 20: 1455-1464
ChEMBL Binding affinity to adrenergic alpha1A receptor (unknown origin) B 9.23 pKi 0.59 nM Ki Med Chem Res (2011) 20: 1455-1464
ChEMBL The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cells B 9.24 pKi 0.58 nM Ki J. Med. Chem. (1999) 42: 173-177 [PMID:9888842]
ChEMBL Binding affinity was determined for the alpha-1A adrenergic receptor B 9.24 pKi 0.58 nM Ki J. Med. Chem. (1998) 41: 5320-5333 [PMID:9857099]
ChEMBL Binding affinity against human Alpha-1A adrenergic receptor B 9.24 pKi 0.58 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 2843-2848 [PMID:10522703]
ChEMBL Binding affinity against Alpha-1A adrenergic receptor from human clone B 9.29 pKi 0.51 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Compound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor B 9.41 pKi 0.39 nM Ki J. Med. Chem. (1998) 41: 1205-1208 [PMID:9548811]
ChEMBL Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor B 9.57 pKi 0.27 nM Ki J. Med. Chem. (1995) 38: 1579-1581 [PMID:7752182]
ChEMBL Binding affinity was tested on human Alpha-1A adrenergic receptor B 9.7 pKi 0.2 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Displacement of [3H]prazosin from alpha1-adrenoceptor (unknown origin) in cerebral cortex membranes after 60 mins by TopCount scintillation counting method B 9.82 pKi 0.15 nM Ki Eur J Med Chem (2018) 144: 701-715 [PMID:29291438]
GtoPdb - - 9.9 pKi - - - Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248];
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358];
FEBS Lett (1998) 422: 279-83 [PMID:9490024];
Br J Pharmacol (1999) 127: 252-8 [PMID:10369480];
Eur J Pharmacol (1999) 370: 337-43 [PMID:10334511]
ChEMBL Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in CHO cells B 10.4 pKi 0.04 nM Ki Eur. J. Med. Chem. (2015) 92: 221-235 [PMID:25557493]
ChEMBL Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells B 10.4 pKi 0.04 nM Ki J. Med. Chem. (2014) 57: 4543-4557 [PMID:24805037]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells B 9.03 pKi 0.93 nM Ki J. Med. Chem. (2003) 46: 265-283 [PMID:12519065]
ChEMBL Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay B 9.14 pKi 0.72 nM Ki J. Med. Chem. (1996) 39: 4602-4607 [PMID:8917649]
ChEMBL Binding affinity against Alpha-1A adrenergic receptor from bovine clone B 9.77 pKi 0.17 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor B 9.9 pKi 0.13 nM Ki J. Med. Chem. (1997) 40: 2674-2687 [PMID:9276013]
Alpha-1a adrenergic receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3637] [UniProtKB: O02824]
ChEMBL Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay F 8.3 pKd 5.01 nM Kd J. Med. Chem. (1997) 40: 2674-2687 [PMID:9276013]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens. F 8.6 pKd 2.51 nM Kd J. Med. Chem. (1998) 41: 4844-4853 [PMID:9822553]
ChEMBL Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat F 8.6 pKd 2.51 nM Kd Bioorg. Med. Chem. Lett. (1998) 8: 1353-1358 [PMID:9871765]
ChEMBL Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor) F 8.98 pKd 1.05 nM Kd J. Med. Chem. (2005) 48: 28-31 [PMID:15633998]
ChEMBL Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips B 9.81 pKd 0.15 nM Kd J. Med. Chem. (1995) 38: 4944-4949 [PMID:8523408]
ChEMBL Compound was tested for its binding affinity towards Alpha-1A adrenergic receptor using [3H]prazosin from rat submaxillary gland B 8.98 pKi 1.05 nM Ki J. Med. Chem. (1998) 41: 1557-1560 [PMID:9572880]
ChEMBL Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay B 9.03 pKi 0.93 nM Ki J. Med. Chem. (1996) 39: 4602-4607 [PMID:8917649]
GtoPdb - - 9.5 pKi - - - J Biol Chem (2001) 276: 25366-71 [PMID:11331292]
ChEMBL Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor B 9.52 pKi 0.3 nM Ki J. Med. Chem. (1998) 41: 1205-1208 [PMID:9548811]
ChEMBL Displacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 mins B 9.55 pKi 0.28 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes B 9.64 pKi 0.23 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 4045-4047 [PMID:16723224]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 10.06 pKi 0.09 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland B 10.15 pKi 0.07 nM Ki J. Med. Chem. (1999) 42: 5181-5187 [PMID:10602703]
ChEMBL Displacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 mins B 9.16 pIC50 0.69 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 9.66 pIC50 0.22 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 Displacement of [125I]HEAT from adrenergic alpha1B receptor (unknown origin) B 8.1 pKi 7.94 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [125I]HEAT from adrenergic alpha1B receptor (unknown origin) B 9 pKi 1 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 576-579 [PMID:24365159]
ChEMBL In vitro binding affinity against Alpha-1B adrenergic receptor of human liver microsomes. B 9.22 pKi 0.6 nM Ki J. Med. Chem. (1999) 42: 4778-4793 [PMID:10579841]
ChEMBL Binding affinity was determined for the alpha-1B adrenergic receptor B 9.26 pKi 0.55 nM Ki J. Med. Chem. (1998) 41: 5320-5333 [PMID:9857099]
ChEMBL Binding affinity against human Alpha-1B adrenergic receptor B 9.26 pKi 0.55 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 2843-2848 [PMID:10522703]
ChEMBL Compound was tested for binding affinity against cloned Alpha-1B adrenergic receptor from hamster smooth muscle using radioligand ([3H]prazosin) binding assay B 9.34 pKi 0.46 nM Ki J. Med. Chem. (1996) 39: 4602-4607 [PMID:8917649]
ChEMBL Binding affinity towards human cloned alpha-1B-adrenoceptor using [3H]prazosin as radioligand B 9.38 pKi 0.42 nM Ki J. Med. Chem. (2001) 44: 2403-2410 [PMID:11448222]
ChEMBL Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1b expressed in CHO cells B 9.39 pKi 0.41 nM Ki J. Med. Chem. (2005) 48: 28-31 [PMID:15633998]
ChEMBL Binding affinity at human cloned Alpha-1B adrenergic receptor in chinese hamster ovary cells by [3H]prazosin displacement. B 9.39 pKi 0.41 nM Ki J. Med. Chem. (1998) 41: 4844-4853 [PMID:9822553]
ChEMBL Displacement of [3H]prazosin from human alpha1B adrenoceptor expressed in CHO cell membranes after 30 mins B 9.39 pKi 0.41 nM Ki Eur J Med Chem (2017) 136: 259-269 [PMID:28499171]
ChEMBL Binding affinity measured in CHO cells expressing human cloned Alpha-1B adrenergic receptor expressed as pKi B 9.39 pKi 0.41 nM Ki J. Med. Chem. (2003) 46: 4895-4903 [PMID:14584940]
ChEMBL Binding affinity against Alpha-1B adrenergic receptor from hamster clones. B 9.49 pKi 0.32 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Binding affinity against Alpha-1B adrenergic receptor from human clone B 9.49 pKi 0.32 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1B adrenergic receptor in CHO cells B 9.55 pKi 0.28 nM Ki J. Med. Chem. (1999) 42: 173-177 [PMID:9888842]
ChEMBL Binding affinity was tested on human Alpha-1B adrenergic receptor B 9.6 pKi 0.25 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Compound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1B adrenergic receptor B 9.68 pKi 0.21 nM Ki J. Med. Chem. (1998) 41: 1205-1208 [PMID:9548811]
ChEMBL Ability to displace [3H]prazosin from cloned human Alpha-1B adrenergic receptor B 9.68 pKi 0.21 nM Ki J. Med. Chem. (1995) 38: 1579-1581 [PMID:7752182]
GtoPdb - - 9.9 pKi - - - Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248];
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358];
Br J Pharmacol (1999) 127: 252-8 [PMID:10369480]
Alpha-1b adrenergic receptor in Hamster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3122] [UniProtKB: P18841]
ChEMBL Displacement of [3H]prazosin (0.5 nM) from hamster Alpha-1B adrenergic receptor expressed in rat-1 cells B 9.08 pKi 0.83 nM Ki J. Med. Chem. (2003) 46: 265-283 [PMID:12519065]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL Antagonism of phenylephrine stimulated contraction of the rat isolated spleen. F 8.99 pKd 1.02 nM Kd J. Med. Chem. (1998) 41: 4844-4853 [PMID:9822553]
ChEMBL Antagonistic affinity against Alpha-1B adrenergic receptor was determined in isolated spleen tissue from rat F 8.99 pKd 1.02 nM Kd Bioorg. Med. Chem. Lett. (1998) 8: 1353-1358 [PMID:9871765]
ChEMBL Blocking activity was assessed by antagonism of (-)-phenylephrine induced contraction of rat spleen (alpha1B adrenoceptor) F 9.01 pKd 0.98 nM Kd J. Med. Chem. (2005) 48: 28-31 [PMID:15633998]
ChEMBL Compound was tested for its binding affinity towards Alpha-1B adrenergic receptor using [3H]prazosin from rat liver B 8.53 pKi 2.93 nM Ki J. Med. Chem. (1998) 41: 1557-1560 [PMID:9572880]
ChEMBL Displacement of [3H]prazosin from rat liver adrenergic alpha1B receptor after 45 mins by liquid scintillation counter B 9.26 pKi 0.55 nM Ki Eur. J. Med. Chem. (2011) 46: 3000-3012 [PMID:21549456]
ChEMBL Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1B adrenergic receptor B 9.7 pKi 0.2 nM Ki J. Med. Chem. (1998) 41: 1205-1208 [PMID:9548811]
ChEMBL Inhibition of [3H]- prazosin binding against Alpha-1B adrenergic receptor from rat liver B 9.82 pKi 0.15 nM Ki J. Med. Chem. (1999) 42: 5181-5187 [PMID:10602703]
ChEMBL Displacement of [3H]Prazosin from alpha1B adrenergic receptor in Wistar rat liver after 60 mins B 9.82 pKi 0.15 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Displacement of [3H]prazosin from adrenergic alpha-1B receptor in rat liver membranes B 10 pKi 0.1 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 4045-4047 [PMID:16723224]
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 10