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 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]
