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ChEMBL ligand: CHEMBL56 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
ChEMBL | Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand | B | 5.76 | pKi | 1757.2 | nM | Ki | J Med Chem (2001) 44: 2403-2410 [PMID:11448222] |
ChEMBL | Binding affinity was determined on human cloned Alpha-1A adrenoceptor | B | 5.76 | pKi | 1757 | nM | Ki | J Med Chem (2001) 44: 4431-4442 [PMID:11728188] |
ChEMBL | The binding affinity was evaluated on cloned human alpha-1A adrenergic receptor expressed in chinese hamster ovary(CHO) cells by using [3H]prazosin as radioligand. | B | 6 | pKi | <6 | nM | Log Ki | J Med Chem (1999) 42: 2961-2968 [PMID:10425105] |
ChEMBL | Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1999) 42: 4214-4224 [PMID:10514291] |
ChEMBL | Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2008) 51: 6359-6370 [PMID:18817363] |
ChEMBL | Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2013) 56: 584-588 [PMID:23252794] |
ChEMBL | Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay | B | 6 | pKi | >1000 | nM | Ki | Eur J Med Chem (2019) 168: 461-473 [PMID:30844609] |
ChEMBL | Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells | B | 6.82 | pKi | 151.36 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 2017-2020 [PMID:20185311] |
ChEMBL | Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting | B | 6.82 | pKi | 151.36 | nM | Ki | J Med Chem (2012) 55: 23-36 [PMID:22145629] |
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130] | ||||||||
ChEMBL | Binding affinity against alpha-1 adrenergic receptor in calf frontal cortex | B | 4.52 | pIC50 | 30000 | nM | IC50 | J Med Chem (1994) 37: 1779-1793 [PMID:7912735] |
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
ChEMBL | In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens. | B | 5.68 | pKi | 2082 | nM | Ki | J Med Chem (2004) 47: 1900-1918 [PMID:15055991] |
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
ChEMBL | Binding affinity towards human cloned alpha-1B-adrenoceptor using [3H]prazosin as radioligand | B | 5.22 | pKi | 5975 | nM | Ki | J Med Chem (2001) 44: 2403-2410 [PMID:11448222] |
ChEMBL | Binding affinity was determined on human cloned alpha-1B adrenergic receptor | B | 5.22 | pKi | 5975 | nM | Ki | J Med Chem (2001) 44: 4431-4442 [PMID:11728188] |
ChEMBL | Binding affinity constant against alpha-1B adrenergic receptor of guinea pig spleen | B | 5.73 | pKi | 1882 | nM | Ki | J Med Chem (2004) 47: 1900-1918 [PMID:15055991] |
ChEMBL | The binding affinity was evaluated on cloned human alpha-1B adrenergic receptor expressed in chinese hamster ovary(CHO) cells by using [3H]prazosin as radioligand. | B | 6 | pKi | <6 | nM | Log Ki | J Med Chem (1999) 42: 2961-2968 [PMID:10425105] |
ChEMBL | Displacement of [3H]prazosin from human recombinant alpha1B adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2012) 55: 23-36 [PMID:22145629] |
ChEMBL | Displacement of [3H]prazosin from human recombinant alpha1B adrenergic receptor expressed in CHO cell membranes after 30 mins | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2013) 56: 584-588 [PMID:23252794] |
ChEMBL | Displacement of [3H]prazosin from human cloned Alpha-1B adrenergic receptor | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1999) 42: 4214-4224 [PMID:10514291] |
ChEMBL | Displacement of [3H]Prazosin from human recombinant alpha 1B adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay | B | 6 | pKi | >1000 | nM | Ki | Eur J Med Chem (2019) 168: 461-473 [PMID:30844609] |
ChEMBL | Displacement of [3H]prazosin from human cloned Alpha-1B adrenoceptor expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2008) 51: 6359-6370 [PMID:18817363] |
ChEMBL | Displacement of [3H]prazosin from human Alpha-1B adrenergic receptor expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 2017-2020 [PMID:20185311] |
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
ChEMBL | The binding affinity was evaluated on cloned human alpha-1D adrenergic receptor expressed in chinese hamster ovary(CHO) cells by using [3H]prazosin as radioligand. | B | 6 | pKi | <6 | nM | Log Ki | J Med Chem (1999) 42: 2961-2968 [PMID:10425105] |
ChEMBL | Displacement of [3H]prazosin from human cloned Alpha-1D adrenergic receptor | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1999) 42: 4214-4224 [PMID:10514291] |
ChEMBL | Binding affinity towarda alpha-1D adrenergic receptor | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2001) 44: 4431-4442 [PMID:11728188] |
ChEMBL | Binding affinity towards human cloned alpha-1D-adrenoceptor using [3H]prazosin as radioligand | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2001) 44: 2403-2410 [PMID:11448222] |
ChEMBL | Displacement of [3H]prazosin from human cloned alpha1D adrenoceptor expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2008) 51: 6359-6370 [PMID:18817363] |
ChEMBL | Displacement of [3H]prazosin from human Alpha-1D adrenergic receptor expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 2017-2020 [PMID:20185311] |
ChEMBL | Displacement of [3H]prazosin from human recombinant Alpha-1D adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2012) 55: 23-36 [PMID:22145629] |
ChEMBL | Displacement of [3H]prazosin from human recombinant alpha1D adrenergic receptor expressed in CHO cell membranes after 30 mins | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2013) 56: 584-588 [PMID:23252794] |
ChEMBL | Displacement of [3H]Prazosin from human recombinant alpha 1D adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay | B | 6 | pKi | >1000 | nM | Ki | Eur J Med Chem (2019) 168: 461-473 [PMID:30844609] |
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944] | ||||||||
ChEMBL | Binding affinity to the adrenergic receptor alpha-1D of rat aorta | B | 5.27 | pKi | 5421 | nM | Ki | J Med Chem (2004) 47: 1900-1918 [PMID:15055991] |
Alpha-2a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4744] [UniProtKB: Q28838] | ||||||||
ChEMBL | Binding affinity against alpha-2 adrenergic receptor in calf frontal cortex | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (1994) 37: 1779-1793 [PMID:7912735] |
Dopamine D1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136] | ||||||||
ChEMBL | Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum | B | 4.06 | pKi | 87300 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
D1 receptor/Dopamine D1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3071] [GtoPdb: 214] [UniProtKB: Q61616] | ||||||||
ChEMBL | Binding affinity against Dopamine receptor D1 | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
ChEMBL | In vitro binding activity against dopamine D1 receptor from homogenized rat brain, using [3H]SCH-23390 as the radioligand | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1989) 32: 2273-2276 [PMID:2571729] |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | Inhibitory activity against [125I]- NCQ298 binding to dopamine receptor D2 in Sf 9 cells | B | 5.49 | pKi | 3243 | nM | Ki | J Med Chem (1993) 36: 3161-3165 [PMID:8230102] |
ChEMBL | Binding affinity against [3H]U-86,170-labeled dopamine receptor D2 in cloned CHO cells | B | 7.07 | pKi | 86 | nM | Ki | J Med Chem (1993) 36: 1053-1068 [PMID:8097537] |
ChEMBL | Binding affinity against [3H]U-86,170-labeled dopamine receptor D2 in cloned CHO cells | B | 7.07 | pKi | 86 | nM | Ki | J Med Chem (1993) 36: 1069-1083 [PMID:8097538] |
ChEMBL | Binding affinity against Dopamine receptor D2 | B | 7.08 | pKi | 84 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
ChEMBL | Inhibitory concentration against binding of Dopamine receptor D2 by displacement of [3H]spiperone | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 509-512 [PMID:10743959] |
Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288] | ||||||||
ChEMBL | Inhibition of [3H]raclopride binding to Dopamine receptor D2 of bovine striatum | B | 5.62 | pKi | 2380 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
ChEMBL | Compound was evaluated for the binding affinity towards Dopamine receptor D2 using [3H]raclopride radioligand. | B | 6.1 | pIC50 | 800 | nM | IC50 | J Med Chem (1996) 39: 4285-4298 [PMID:8863806] |
ChEMBL | Binding affinity against D2 receptor in calf caudate nucleus | B | 6.1 | pIC50 | 800 | nM | IC50 | J Med Chem (1994) 37: 1779-1793 [PMID:7912735] |
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
ChEMBL | Binding affinity of compound against Dopamine receptor D2 binding site using radioligand [3H]spiperone | B | 5.46 | pKi | 3500 | nM | Ki | J Med Chem (1989) 32: 1959-1962 [PMID:2569041] |
ChEMBL | Binding affinity against D2 receptor in homogenated rat brain tissue, using by [3H]spiperone as radioligand | B | 5.87 | pKi | 1357 | nM | Ki | J Med Chem (1993) 36: 3409-3416 [PMID:8230131] |
ChEMBL | Displacement of [3H]spiperone from dopamine receptor D2 | B | 5.87 | pKi | 1357 | nM | Ki | J Med Chem (1993) 36: 2059-2065 [PMID:8340910] |
ChEMBL | Displacement of the radioligand [3H]spiperone from D2 receptor | B | 5.87 | pKi | 1357 | nM | Ki | J Med Chem (1994) 37: 3263-3273 [PMID:7932553] |
ChEMBL | Binding affinity against Dopamine receptor D2 from CHO-K1 cells, using [3H]U-86,170 as the radioligand. | B | 5.95 | pKi | 1126 | nM | Ki | J Med Chem (1995) 38: 2202-2216 [PMID:7783152] |
ChEMBL | The binding affinity was evaluated on Dopamine receptor D2 expressed in rat striatum by using [3H]spiperone as radioligand | B | 6 | pKi | <6 | nM | Log Ki | J Med Chem (1999) 42: 2961-2968 [PMID:10425105] |
ChEMBL | Binding affinity against [3H]raclopride-labeled dopamine receptor D2 in rat striatum. | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1993) 36: 1053-1068 [PMID:8097537] |
ChEMBL | Displacement of [3H]spiperone from rat brain Dopamine receptor D2 | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1999) 42: 4214-4224 [PMID:10514291] |
ChEMBL | Binding affinity for [3H]raclopride-labeled dopamine receptor D2 in rat striatum | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1993) 36: 1069-1083 [PMID:8097538] |
ChEMBL | Displacement of [3H]YM-09151-2 from rat striatum D2 receptor | B | 6.26 | pKi | 549.54 | nM | Ki | J Med Chem (2007) 50: 865-876 [PMID:17300168] |
ChEMBL | Displacement of [3H]U-86170 from Dopamine receptor D2 | B | 7.07 | pKi | 86 | nM | Ki | J Med Chem (1995) 38: 725-734 [PMID:7861420] |
ChEMBL | Tested in vitro for the inhibition of [3H]raclopride binding to Dopamine receptor D2 in rat striatum | B | 7.07 | pKi | 86 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2759-2764 |
ChEMBL | The compound was tested in vitro for inhibitory activity against dopamine receptor in rats using [3H]spiperone as radioligand | B | 5.24 | pIC50 | 5800 | nM | IC50 | J Med Chem (1992) 35: 3984-3990 [PMID:1433207] |
ChEMBL | In vitro binding activity against Dopamine receptor D2 from homogenized rat brain, using [3H]spiperone as the radioligand | B | 5.24 | pIC50 | 5760 | nM | IC50 | J Med Chem (1989) 32: 2273-2276 [PMID:2571729] |
ChEMBL | Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand | B | 8.28 | pIC50 | 5.2 | nM | IC50 | J Med Chem (1996) 39: 3195-3202 [PMID:8759642] |
ChEMBL | Binding affinity towards rat Dopamine receptor D2 was evaluated using [3H]- spiroperidol as radioligand | B | 8.28 | pIC50 | 5.2 | nM | IC50 | J Med Chem (1996) 39: 4928-4934 [PMID:8960552] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
ChEMBL | Inhibition of [3H]spiperone binding to Dopamine receptor D3 in bovine cortex | B | 4.84 | pKi | 14600 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
ChEMBL | Tested in vitro for the inhibition of [3H]U-86170 binding to Dopamine receptor D3, expressed in cloned CHO cells | B | 6.59 | pKi | 259 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2759-2764 |
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
ChEMBL | Binding affinity against Dopamine receptor D3 from CHO-K1 cells, using [3H]spiperone as the radioligand. | B | 6.48 | pKi | 333 | nM | Ki | J Med Chem (1995) 38: 2202-2216 [PMID:7783152] |
ChEMBL | Inhibitory activity against [125I]- NCQ298 binding to dopamine receptor D3 in Sf 9 cells | B | 6.6 | pKi | 251 | nM | Ki | J Med Chem (1993) 36: 3161-3165 [PMID:8230102] |
ChEMBL | Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. | B | 6.61 | pKi | 248 | nM | Ki | J Med Chem (1993) 36: 1499-1500 [PMID:8098771] |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
ChEMBL | Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells | B | 5.82 | pKi | >1515 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2759-2764 |
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
ChEMBL | Binding affinity against dopamine transporter (DAT) by displacement of [3H]WIN-35428 in male wistar rats | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] | ||||||||
ChEMBL | Binding affinity against norepinephrine transporter (NET) by displacement of [3H]nisoxetine in male wistar rats | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
GtoPdb | - | - | 9.4 | pKd | 0.4 | nM | Kd |
Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 447-53 [PMID:10431754]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 205-17 [PMID:9550290]; Biosci Rep (2004) 24: 101-15 [PMID:15628665]; J Med Chem (2000) 43: 4701-10 [PMID:11101361] |
ChEMBL | Displacement of [3H]WAY100635 from human recombinant 5HT1A receptor | B | 5.4 | pKi | 3981.07 | nM | Ki | J Med Chem (2008) 51: 2887-2890 [PMID:18433113] |
ChEMBL | Displacement of [3H]8-OH-DPAT from human cloned 5-HT1A receptor expressed in human HeLa cells | B | 5.48 | pKi | 3300 | nM | Ki | J Med Chem (2008) 51: 7602-7613 [PMID:19053888] |
ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells after 120 mins | B | 8.29 | pKi | 5.1 | nM | Ki | J Med Chem (2008) 51: 1492-1495 [PMID:18269229] |
ChEMBL | Binding affinity to human 5-hydroxytryptamine 1A receptor was measured using [3H]-8-hydroxy-2-(di-n-propylamine) tetraline [3H]8-OH-DPAT) as radioligand | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (2004) 47: 1900-1918 [PMID:15055991] |
ChEMBL | Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor expressed in human HeLa cells |