terazosin [Ligand Id: 7302] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL611 (Terazosin, Hytrin)
  • 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]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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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 In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate F 7.44 pKd 36.31 nM Kd J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
ChEMBL In vitro antagonistic activity against alpha-1A receptor in dog prostate. F 7.44 pKd 36.31 nM Kd J. Med. Chem. (2001) 44: 1971-1985 [PMID:11384242]
ChEMBL Binding affinity was tested on human Alpha-1A adrenergic receptor B 7.4 pKi 39.81 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog prostate tissue preparations B 7.49 pKi 32 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 2467-2472 [PMID:9873563]
ChEMBL Binding affinity against Alpha-1A adrenergic receptor from human clone B 8.14 pKi 7.3 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor B 8.16 pKi 6.92 nM Ki J. Med. Chem. (1998) 41: 2643-2650 [PMID:9651170]
ChEMBL In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes. B 8.16 pKi 6.9 nM Ki J. Med. Chem. (1999) 42: 4794-4803 [PMID:10579842]
ChEMBL Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor B 8.16 pKi 6.9 nM Ki J. Med. Chem. (1995) 38: 1579-1581 [PMID:7752182]
ChEMBL In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes B 8.16 pKi 6.9 nM Ki J. Med. Chem. (1999) 42: 4778-4793 [PMID:10579841]
ChEMBL In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes. B 8.16 pKi 6.9 nM Ki J. Med. Chem. (1999) 42: 4764-4777 [PMID:10579840]
ChEMBL Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor B 8.38 pKi 4.2 nM Ki J. Med. Chem. (1998) 41: 1205-1208 [PMID:9548811]
ChEMBL Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells B 8.38 pKi 4.2 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 2467-2472 [PMID:9873563]
ChEMBL In vitro binding affinity radioligand B 8.4 pKi 4 nM Ki J. Med. Chem. (1999) 42: 4764-4777 [PMID:10579840]
ChEMBL Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in human prostate tissue preparations B 8.54 pKi 2.9 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 2467-2472 [PMID:9873563]
ChEMBL Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in human aorta preparations B 8.62 pKi 2.4 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 2467-2472 [PMID:9873563]
ChEMBL Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog aorta preparations B 8.7 pKi 2 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 2467-2472 [PMID:9873563]
ChEMBL Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand B 8.7 pKi 2 nM Ki J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
GtoPdb - - 8.7 pKi 2 nM Ki J. Med. Chem. (1997) 40: 3141-3 [PMID:9379432]
ChEMBL Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay B 7.28 pEC50 51.89 nM EC50 Bioorg Med Chem (2016) 24: 5582-5591 [PMID:27658792]
ChEMBL Antagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay B 7.29 pEC50 51 nM EC50 Bioorg. Med. Chem. (2015) 23: 2104-2111 [PMID:25813897]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Binding affinity against Alpha-1A adrenergic receptor from bovine clone B 7.59 pKi 26 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 8.6 pKi 2.51 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 7.7 pKd 19.95 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 Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins B 7.9 pKd 12.59 nM Kd Eur. J. Med. Chem. (2015) 96: 83-91 [PMID:25874333]
ChEMBL Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response F 7.9 pKd 12.59 nM Kd Bioorg Med Chem Lett (2018) 28: 547-551 [PMID:29422390]
ChEMBL In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens F 8.04 pKd 9.12 nM Kd J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
ChEMBL In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens F 8.04 pKd 9.12 nM Kd J. Med. Chem. (2001) 44: 1971-1985 [PMID:11384242]
ChEMBL Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of phenylephrine-induced contractile response F 8.04 pKd 9.12 nM Kd Bioorg Med Chem Lett (2018) 28: 547-551 [PMID:29422390]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 8.02 pKi 9.59 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor B 8.41 pKi 3.9 nM Ki J. Med. Chem. (1998) 41: 1205-1208 [PMID:9548811]
ChEMBL In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A B 9.09 pKi 0.82 nM Ki J. Med. Chem. (2000) 43: 1586-1603 [PMID:10780916]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 7.62 pIC50 24 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 Binding affinity against Alpha-1B adrenergic receptor from hamster clones. B 7.52 pKi 30 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Binding affinity against human adrenergic receptor subtype Alpha-1B adrenergic receptor using [3H]prazosin as radioligand B 8.57 pKi 2.68 nM Ki J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
ChEMBL Ability to displace [3H]prazosin from cloned human Alpha-1B adrenergic receptor B 8.59 pKi 2.6 nM Ki J. Med. Chem. (1995) 38: 1579-1581 [PMID:7752182]
ChEMBL Binding affinity was tested on human Alpha-1B adrenergic receptor B 8.6 pKi 2.51 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
GtoPdb - - 8.6 pKi 2.68 nM Ki J. Med. Chem. (1997) 40: 3141-3 [PMID:9379432]
ChEMBL Binding affinity against Alpha-1B adrenergic receptor from human clone B 8.66 pKi 2.2 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Binding affinity determined by displacement of [3H]prazosin from alpha-1B adrenergic receptor B 8.71 pKi 1.95 nM Ki J. Med. Chem. (1998) 41: 2643-2650 [PMID:9651170]
ChEMBL In vitro binding affinity against Alpha-1B adrenergic receptor of human liver microsomes. B 8.72 pKi 1.9 nM Ki J. Med. Chem. (1999) 42: 4764-4777 [PMID:10579840]
ChEMBL In vitro binding affinity against Alpha-1B adrenergic receptor of human liver microsomes. B 8.72 pKi 1.9 nM Ki J. Med. Chem. (1999) 42: 4794-4803 [PMID:10579842]
ChEMBL Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1b adrenergic receptor stably expressed in LM cells B 8.92 pKi 1.2 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 2467-2472 [PMID:9873563]
ChEMBL Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1B adrenergic receptor B 8.92 pKi 1.2 nM Ki J. Med. Chem. (1998) 41: 1205-1208 [PMID:9548811]
ChEMBL Antagonist activity at alpha-1B adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay B 9.3 pEC50 0.5 nM EC50 Bioorg. Med. Chem. (2015) 23: 2104-2111 [PMID:25813897]
Alpha-1b adrenergic receptor in Hamster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3122] [UniProtKB: P18841]
ChEMBL In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1b expressed in LTK cell B 9.16 pKi 0.69 nM Ki J. Med. Chem. (2000) 43: 1586-1603 [PMID:10780916]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL Antagonist activity at Sprague-Dawley rat spleen adrenergic alpha-1B receptor after 20 mins B 8.59 pKd 2.57 nM Kd Eur. J. Med. Chem. (2015) 96: 83-91 [PMID:25874333]
ChEMBL Antagonist activity at alpha1B-adrenoreceptor in Sprague-Dawley rat spleen assessed as relaxation of (-)-noradrenaline-induced contractile response F 8.59 pKd 2.57 nM Kd Bioorg Med Chem Lett (2018) 28: 547-551 [PMID:29422390]
ChEMBL In vitro antagonism against Alpha-1B adrenergic receptor using phenylephrine (PE) challenge in rat spleen F 8.6 pKd 2.51 nM Kd J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
ChEMBL In vitro antagonistic activity against alpha-1B receptor in rat spleen. F 8.6 pKd 2.51 nM Kd J. Med. Chem. (2001) 44: 1971-1985 [PMID:11384242]
ChEMBL Antagonist activity at alpha1B-adrenoreceptor in Sprague-Dawley rat spleen assessed as relaxation of phenylephrine-induced contractile response F 8.6 pKd 2.51 nM Kd Bioorg Med Chem Lett (2018) 28: 547-551 [PMID:29422390]
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 8.48 pKi 3.33 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1B adrenergic receptor B 8.72 pKi 1.9 nM Ki J. Med. Chem. (1998) 41: 1205-1208 [PMID:9548811]
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 8.22 pIC50 6.03 nM IC50 DrugMatrix in vitro pharmacology data
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 8.08 pKi 8.36 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity was tested on human Alpha-1D adrenergic receptor B 8.4 pKi 3.98 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 8.43 pKi 3.7 nM Ki J. Med. Chem. (1995) 38: 1579-1581 [PMID:7752182]
ChEMBL Binding affinity against Alpha-1D adrenergic receptor, from human clones. B 8.46 pKi 3.5 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL In vitro binding affinity against Alpha-1D adrenergic receptor of human liver microsomes. B 8.46 pKi 3.5 nM Ki J. Med. Chem. (1999) 42: 4764-4777 [PMID:10579840]
ChEMBL In vitro binding affinity against Alpha-1D adrenergic receptor of human liver microsomes. B 8.46 pKi 3.5 nM Ki J. Med. Chem. (1999) 42: 4794-4803 [PMID:10579842]
ChEMBL Binding affinity determined by displacement of [3H]prazosin from alpha-1D adrenergic receptor B 8.46 pKi 3.47 nM Ki J. Med. Chem. (1998) 41: 2643-2650 [PMID:9651170]
ChEMBL Ability to displace beta ([125I]-iodo-4-hydroxyphenyl) ethylamino methyl tetralone from human cloned Alpha-1d adrenergic receptor stably expressed in HEK cells. B 8.7 pKi 2 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 2467-2472 [PMID:9873563]
ChEMBL Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1D adrenergic receptor B 8.7 pKi 2 nM Ki J. Med. Chem. (1998) 41: 1205-1208 [PMID:9548811]
ChEMBL Binding affinity against human adrenergic receptor subtype Alpha-1D adrenergic receptor using [3H]prazosin as radioligand B 9.07 pKi 0.85 nM Ki J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
GtoPdb - - 9.1 pKi 0.85 nM Ki J. Med. Chem. (1997) 40: 3141-3 [PMID:9379432]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 7.77 pIC50 17 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 antagonism against Alpha-1D adrenergic receptor using phenylephrine (PE) challenge in rat aorta F 8.65 pKd 2.24 nM Kd J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
ChEMBL Antagonist activity at alpha1D-adrenoreceptor in Sprague-Dawley rat thoracic aorta assessed as relaxation of phenylephrine-induced contractile response F 8.65 pKd 2.24 nM Kd Bioorg Med Chem Lett (2018) 28: 547-551 [PMID:29422390]
ChEMBL Antagonist activity at Sprague-Dawley rat thoracic aorta adrenergic alpha-1D receptor after 20 mins B 8.83 pKd 1.48 nM Kd Eur. J. Med. Chem. (2015) 96: 83-91 [PMID:25874333]
ChEMBL Antagonist activity at alpha1D-adrenoreceptor in Sprague-Dawley rat thoracic aorta assessed as relaxation of (-)-noradrenaline-induced contractile response F 8.83 pKd 1.48 nM Kd Bioorg Med Chem Lett (2018) 28: 547-551 [PMID:29422390]
ChEMBL Binding affinity against Alpha-1D adrenergic receptor, from rat clones. B 7.46 pKi 35 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 8.47 pKi 3.4 nM Ki J. Med. Chem. (1998) 41: 1205-1208 [PMID:9548811]
ChEMBL In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1d expressed in LTK cell B 9 pKi 1.01 nM Ki J. Med. Chem. (2000) 43: 1586-1603 [PMID:10780916]
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 5.29 pKi 5187 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity against Alpha-2A adrenergic receptor, from human clones. B 5.43 pKi 3702 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand B 5.82 pKi 1500 nM Ki J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
ChEMBL Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor B 6.26 pKi 550 nM Ki J. Med. Chem. (1995) 38: 1579-1581 [PMID:7752182]
ChEMBL Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor B 6.26 pKi 549.54 nM Ki J. Med. Chem. (1998) 41: 2643-2650 [PMID:9651170]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 4.86 pIC50 13832 nM IC50 DrugMatrix in vitro pharmacology data
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 6.38 pKi 418 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 6.71 pKi 195 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity determined by displacement of [3H]rauwolscine from alpha-2B adrenergic receptor B 7.51 pKi 30.9 nM Ki J. Med. Chem. (1998) 41: 2643-2650 [PMID:9651170]
ChEMBL Ability to displace [3H]rauwolscine from cloned human Alpha-2B adrenergic receptor B 7.59 pKi 26 nM Ki J. Med. Chem. (1995) 38: 1579-1581 [PMID:7752182]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 6.37 pIC50 428 nM IC50 DrugMatrix in vitro pharmacology data
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
ChEMBL Binding affinity against rat Alpha-2B adrenergic receptor using [3H]rauwolscine as radioligand B 8.11 pKi 7.7 nM Ki J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 6.06 pKi 878 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptor B 6.65 pKi 223.87 nM Ki J. Med. Chem. (1998) 41: 2643-2650 [PMID:9651170]
ChEMBL The compound was tested for binding affinity against alpha-2C-adrenoceptor, from human clones. B 6.67 pKi 213 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor B 6.77 pKi 170 nM Ki J. Med. Chem. (1995) 38: 1579-1581 [PMID:7752182]
ChEMBL Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligand B 7.11 pKi 78 nM Ki J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 5.22 pIC50 6042 nM IC50 DrugMatrix in vitro pharmacology data
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 4.75 pIC50 17782.79 nM IC50 Eur. J. Med. Chem. (2011) 46: 618-630 [PMID:21185626]
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 4.63 pIC50 23700 nM IC50 J. Med. Chem. (2008) 51: 5932-5942 [PMID:18788725]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]