prazosin [Ligand Id: 503] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| 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]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| 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 | pKi | 0.1 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Displacement of [3H]prazosin from rat liver adrenergic alpha1B receptor after 45 mins by liquid scintillation counter | B | 9.07 | pIC50 | 0.85 | nM | IC50 | Eur J Med Chem (2011) 46: 3000-3012 [PMID:21549456] |
| ChEMBL | Displacement of [3H]Prazosin from alpha1B adrenergic receptor in Wistar rat liver after 60 mins | B | 9.57 | pIC50 | 0.27 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
| ChEMBL | DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) | B | 9.75 | pIC50 | 0.18 | 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 | Displacement of [125I]HEAT from adrenergic alpha1D receptor (unknown origin) | B | 9.34 | pKi | 0.46 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
| ChEMBL | Displacement of [3H]Prazosin from human recombinant alpha1D adrenergic receptor expressed in HEK293 cells after 60 mins | B | 9.37 | pKi | 0.43 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
| ChEMBL | Displacement of [125I]HEAT from adrenergic alpha1D receptor (unknown origin) | B | 9.38 | pKi | 0.42 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
| ChEMBL | Binding affinity against human Alpha-1D adrenergic receptor (h alpha-1d) | B | 9.48 | pKi | 0.33 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2843-2848 [PMID:10522703] |
| ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 9.49 | pKi | 0.32 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Binding affinity against Alpha-1D adrenergic receptor, from human clones. | B | 9.49 | pKi | 0.32 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
| ChEMBL | Binding affinity was tested on human Alpha-1D adrenergic receptor | B | 9.5 | pKi | 0.32 | nM | Ki | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
| ChEMBL | Ability to displace [3H]prazosin from cloned human Alpha-1D adrenergic receptor | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (1995) 38: 1579-1581 [PMID:7752182] |
| ChEMBL | In vitro binding affinity against alpha-1D adrenergic receptor of human liver microsomes. | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (1999) 42: 4778-4793 [PMID:10579841] |
| ChEMBL | The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1D adrenergic receptor in CHO cells | B | 9.54 | pKi | 0.29 | nM | Ki | J Med Chem (1999) 42: 173-177 [PMID:9888842] |
| ChEMBL | Binding affinity towards human cloned alpha-1D-adrenoceptor using [3H]prazosin as radioligand | B | 9.64 | pKi | 0.23 | 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 1d expressed in CHO cells | B | 9.65 | pKi | 0.22 | nM | Ki | J Med Chem (2005) 48: 28-31 [PMID:15633998] |
| ChEMBL | Binding affinity measured in CHO cells expressing human cloned Alpha-1D adrenergic receptor expressed as pKi | B | 9.65 | pKi | 0.22 | nM | Ki | J Med Chem (2003) 46: 4895-4903 [PMID:14584940] |
| ChEMBL | Binding affinity at human cloned Alpha-1D adrenergic receptor in chinese hamster ovary cells by [3H]prazosin displacement. | B | 9.65 | pKi | 0.22 | nM | Ki | J Med Chem (1998) 41: 4844-4853 [PMID:9822553] |
| ChEMBL | Displacement of [3H]prazosin from human alpha1D adrenoceptor expressed in CHO cell membranes after 30 mins | B | 9.65 | pKi | 0.22 | nM | Ki | Eur J Med Chem (2017) 136: 259-269 [PMID:28499171] |
| ChEMBL | Compound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1D adrenergic receptor | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (1998) 41: 1205-1208 [PMID:9548811] |
| ChEMBL | Displacement of [3H]prazosin from human recombinant adrenergic alpha-1D receptor expressed in CHO cell membranes incubated for 60 mins | B | 9.77 | pKi | 0.17 | nM | Ki | J Med Chem (2020) 63: 433-439 [PMID:31834797] |
| GtoPdb | - | - | 10.2 | 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]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| ChEMBL | Displacement of [3H]Prazosin from human recombinant alpha1D adrenergic receptor expressed in HEK293 cells after 60 mins | B | 9.06 | pIC50 | 0.88 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
| ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 9.18 | pIC50 | 0.66 | 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 | In vitro antagonist activity against (-)-phenylephrine or (-)-norepinephrine-induced alpha1-adrenoceptor-mediated vasoconstriction of rabbit isolated pulmonary artery. | F | 8.7 | pKd | 2 | nM | Kd | J Med Chem (1984) 27: 495-503 [PMID:6142954] |
| ChEMBL | Antagonism of norepinephrine induced contraction of rat isolated thoracic aorta. | F | 8.91 | pKd | 1.23 | nM | Kd | J Med Chem (1998) 41: 4844-4853 [PMID:9822553] |
| ChEMBL | Antagonistic affinity against Alpha-1D adrenergic receptor was determined in isolated thoracic aorta from rat | F | 8.91 | pKd | 1.23 | 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 thoracic aorta (Alpha-1D adrenoceptor) | F | 9.01 | pKd | 0.98 | nM | Kd | J Med Chem (2005) 48: 28-31 [PMID:15633998] |
| ChEMBL | Antagonist activity at adrenergic alpha 1D receptor in rat thoracic aorta assessed as inhibition of noradrenaline-induced contraction after 1 hr | F | 9.77 | pKd | 0.17 | nM | Kd | Eur J Med Chem (2011) 46: 3000-3012 [PMID:21549456] |
| ChEMBL | Compound was tested for binding affinity against cloned Alpha-1D adrenergic receptor from rat brain. | B | 8.86 | pKi | 1.38 | nM | Ki | J Med Chem (1996) 39: 4602-4607 [PMID:8917649] |
| ChEMBL | Binding affinity against Alpha-1D adrenergic receptor, from rat clones. | B | 9.1 | pKi | 0.79 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
| ChEMBL | Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1D adrenergic receptor | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (1998) 41: 1205-1208 [PMID:9548811] |
| ChEMBL | Displacement of [3H]prazosin (0.3 nM) from rat Alpha-1D adrenergic receptor expressed in CHO cells | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | Binding affinity against Alpha-2A adrenergic receptor, from human clones. | B | 5.67 | pKi | 2133 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 6 | pKi | 989 | nM | Ki | DrugMatrix in vitro pharmacology data |
| GtoPdb | - | - | 6.5 | pKi | - | - | - |
Mol Pharmacol (1992) 42: 1-5 [PMID:1353247]; Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642]; Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| ChEMBL | Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor | B | 6.68 | pKi | 210 | nM | Ki | J Med Chem (1995) 38: 1579-1581 [PMID:7752182] |
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 5.58 | pIC50 | 2638 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Alpha-2a adrenergic receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2350] [UniProtKB: P18871] | ||||||||
| ChEMBL | Compound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-clone | B | 5.39 | pKi | 4100 | 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 | 6.97 | pKi | 106 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909] | ||||||||
| ChEMBL | The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones. | B | 5.78 | pKi | 1668 | 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 | Binding affinity against Alpha-2B adrenergic receptor from human clones. | B | 6.44 | pKi | 365 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
| ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 6.88 | pKi | 133 | nM | Ki | DrugMatrix in vitro pharmacology data |
| GtoPdb | - | - | 7.5 | 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]; Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| ChEMBL | Ability to displace [3H]rauwolscine from cloned human Alpha-2B adrenergic receptor | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (1995) 38: 1579-1581 [PMID:7752182] |
| ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 6.54 | pIC50 | 290 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | Binding affinity against Alpha-2C adrenergic receptor from human clones. | B | 7.02 | pKi | 95 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
| ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 7.03 | pKi | 94 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor | B | 7.62 | pKi | 24 | nM | Ki | J Med Chem (1995) 38: 1579-1581 [PMID:7752182] |
| GtoPdb | - | - | 8 | 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]; Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 6.19 | pIC50 | 647 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Beta casein in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2210] [UniProtKB: P02665] | ||||||||
| ChEMBL | Compound was tested for binding Alpha-1B adrenergic receptor from rat liver using radioligand ([3H]prazosin) binding assay | B | 9.44 | pKi | 0.36 | nM | Ki | J Med Chem (1996) 39: 4602-4607 [PMID:8917649] |
| D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1 | B | 5.25 | pKi | >5600 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | Binding affinity at native Dopamine receptor D2 in rat striatum by [3H]spiperone displacement. | B | 5 | pKi | <10000 | nM | Ki | J Med Chem (1998) 41: 4844-4853 [PMID:9822553] |
| ChEMBL | Antagonistic affinity against rat striatum Dopamine receptor D2 | F | 5 | pKi | <10000 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1353-1358 [PMID:9871765] |
| ChEMBL | Compound was tested for binding affinity against native Dopamine receptor D2 from rat striatum using radioligand [3H]-spiperone) | B | 5 | pKi | <10000 | nM | Ki | J Med Chem (1996) 39: 4602-4607 [PMID:8917649] |
| ChEMBL | Inhibition of [3H]spiperone binding to Dopamine receptor D2 from rat striatal membranes | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (1988) 31: 2247-2256 [PMID:2903929] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Ability to displace [3H]spiperone (0.3 nM) from CHO cells of human Dopamine receptor D3 | B | 5.15 | pKi | >7100 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells | B | 5.08 | pKi | 8300 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) | B | 4.7 | pKi | 19890.2 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) | B | 4.61 | pIC50 | 24277.8 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | Inhibitory concentration against potassium channel HERG | B | 5.8 | pIC50 | 1584.89 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273] |
| ChEMBL | Inhibition of human ERG | B | 5.8 | pIC50 | 1584.89 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
| MMP1/Matrix metalloproteinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956] | ||||||||
| ChEMBL | DRUGMATRIX: Peptidase, Matrix Metalloprotease-1 (MMP-1) enzyme inhibition (substrate: Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2) | B | 5.39 | pIC50 | 4036 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| MMP9/Matrix metalloproteinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780] | ||||||||
| ChEMBL | DRUGMATRIX: Protease, Matrix Metalloprotease-9 (MMP-9) enzyme inhibition (substrate: Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2) | B | 5.16 | pIC50 | 6963 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8] | ||||||||
| ChEMBL | Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 5.8 | pIC50 | 1600 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| MATE2/Multidrug and toxin extrusion protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8] | ||||||||
| ChEMBL | Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 4.42 | pIC50 | 38400 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| Quinone reductase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3959] [UniProtKB: P16083] | ||||||||
| ChEMBL | Binding affinity to low affinity melatonin (MT3) site of quinone reductase 2 | B | 8.11 | pIC50 | 7.8 | nM | IC50 | Eur J Med Chem (2011) 46: 1622-1629 [PMID:21377769] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Ability to displace [3H]5-CT (2.0 nM) from HeLa cells of human 5-hydroxytryptamine 1A receptor | B | 5.74 | pKi | >1800 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| ChEMBL | Binding affinity at native 5-hydroxytryptamine 1A receptor in rat by [3H]8-hydroxy-2-(di-n-propylamino)tetraline displacement. | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1998) 41: 4844-4853 [PMID:9822553] |
| ChEMBL | Antagonistic affinity against cloned human 5-hydroxytryptamine 1A receptor | F | 6 | pKi | <1000 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1353-1358 [PMID:9871765] |
| ChEMBL | Binding affinity towards human cloned 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand | B | 8 | pKi | >10 | nM | Ki | J Med Chem (2001) 44: 2403-2410 [PMID:11448222] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | The compound was tested for binding affinity on [3H]8-OH-DPAT as specific ligand on 5-hydroxytryptamine 1A receptor in rat hippocampus | B | 5.63 | pKi | 2360 | nM | Ki | J Med Chem (1999) 42: 173-177 [PMID:9888842] |
| ChEMBL | Binding affinity against native 5-HT1A-receptors from rat hippocampus using radioligand ([3H]8-hydroxy-2-(di-n-propylamino)-tetraline) binding assay | B | 5.63 | pKi | 2344.23 | nM | Ki | J Med Chem (1996) 39: 4602-4607 [PMID:8917649] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor | B | 5.11 | pKi | >7700 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | Binding affinity was determined for the alpha-1D adrenergic receptor | B | 9.48 | pKi | 0.33 | nM | Ki | J Med Chem (1998) 41: 5320-5333 [PMID:9857099] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| ChEMBL | Displacement of [3H]ketanserin (0.5 nM) from rat cerebral cortex 5-hydroxytryptamine 2A receptors | B | 5.82 | pKi | 1500 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| 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 | 5.58 | pKi | 2621 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 5.39 | pIC50 | 4118 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
| ChEMBL | Ability to displace [3H]mesulergine (0.5 nM) from SR-3T3 cells of rat 5-HT2C receptor | B | 5.38 | pKi | >4200 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245] | ||||||||
| ChEMBL | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy | B | 5 | pIC50 | 9900 | nM | IC50 | J Med Chem (2008) 51: 5932-5942 [PMID:18788725] |
| ChEMBL | TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT1-expressing HEK293 cells | F | 5.74 | pIC50 | 1840 | nM | IC50 | Br J Pharmacol (2002) 136: 829-836 [PMID:12110607] |
| Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT2-expressing HEK293 cells | F | 4 | pIC50 | >100000 | nM | IC50 | Br J Pharmacol (2002) 136: 829-836 [PMID:12110607] |
| ChEMBL | Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay | B | 4.87 | pIC50 | 13600 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| Organic cation transporter 3/Solute carrier family 22 member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT3-expressing HEK293 cells | F | 4.9 | pIC50 | 12600 | nM | IC50 | Br J Pharmacol (2002) 136: 829-836 [PMID:12110607] |
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]
