prazosin [Ligand Id: 503] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2 (CP-12299, CP-122991, Prazosin, Prazosina, Prazosine) |
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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 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]
