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ChEMBL ligand: CHEMBL2 (CP-12299, CP-122991, Prazosin) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 |