terazosin [Ligand Id: 7302] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL611 (Hytrin, Terazosabb, Terazosin) |
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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]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]; J Pharmacol Exp Ther (2019) 371: 106-112 [PMID:31285236] |
| 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 | - | - | - |
J Med Chem (1997) 40: 3141-3 [PMID:9379432]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| 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]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| 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 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]
