8-OH-DPAT [Ligand Id: 7] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL56 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 | 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] | ||||||||
| 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 | B | 8.43 | pKi | 3.71 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 2017-2020 [PMID:20185311] |
| ChEMBL | Displacement of [3H]-OH-DPAT from human recombinant 5HT1A receptor expressed in HeLa cells after 30 mins by liquid scintillation counting | B | 8.43 | pKi | 3.71 | nM | Ki | J Med Chem (2012) 55: 23-36 [PMID:22145629] |
| ChEMBL | Displacement of [3H]8-hydroxy-2-(di-n-propylamino)tetralin from human 5-hydroxytryptamine 1A receptor | B | 8.46 | pKi | 3.47 | nM | Ki | J Med Chem (1999) 42: 4214-4224 [PMID:10514291] |
| ChEMBL | Binding affinity on human cloned 5-hydroxytryptamine 1A receptor transfected in human cell lines(He La) | B | 8.46 | pKi | 3.44 | nM | Ki | J Med Chem (2001) 44: 4431-4442 [PMID:11728188] |
| ChEMBL | Binding affinity towards human cloned 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand | B | 8.46 | pKi | 3.44 | nM | Ki | J Med Chem (2001) 44: 2403-2410 [PMID:11448222] |
| ChEMBL | The binding affinity was evaluated on cloned human 5-hydroxytryptamine 1A receptor expressed in HeLa cells by using DPAT as radioligand. | B | 8.47 | pKi | 8.47 | nM | Log Ki | J Med Chem (1999) 42: 2961-2968 [PMID:10425105] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HeLa cell membranes after 30 mins | B | 8.47 | pKi | 3.39 | nM | Ki | J Med Chem (2013) 56: 584-588 [PMID:23252794] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HeLa cells after 30 mins | B | 8.47 | pKi | 3.39 | nM | Ki | ACS Med Chem Lett (2012) 3: 535-539 [PMID:24900506] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human recombinant 5-HT1A receptor expressed in human HeLa cells incubated for 30 mins by radioligand competition binding assay | B | 8.47 | pKi | 3.39 | nM | Ki | Eur J Med Chem (2019) 168: 461-473 [PMID:30844609] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from recombinant human 5HT1A receptor expressed in human HeLa cell membranes after 30 mins by liquid scintillation counting method | B | 8.47 | pKi | 3.39 | nM | Ki | Eur J Med Chem (2017) 125: 233-244 [PMID:27662034] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in human HeLa cells | B | 8.47 | pKi | 3.39 | nM | Ki | J Med Chem (2008) 51: 6359-6370 [PMID:18817363] |
| ChEMBL | Binding affinity at human 5HT1A receptor | B | 8.47 | pKi | 3.39 | nM | Ki | ACS Med Chem Lett (2013) 4: 875-879 [PMID:24900763] |
| ChEMBL | Displacement of 8-OH-DPAT from human 5-hydroxytryptamine 1A receptor expressed in chinese hamster ovary cells | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2005) 48: 3467-3470 [PMID:15887953] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in CHO cells | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2008) 51: 6980-7004 [PMID:18834188] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from recombinant human 5-HT1A receptor expressed in CHOK1 cell membranes after 1 hr by liquid scintillation counting method | B | 8.58 | pKi | 2.65 | nM | Ki | Bioorg Med Chem (2017) 25: 1250-1259 [PMID:28063784] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry | B | 8.58 | pKi | 2.65 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 4052-4056 [PMID:27396505] |
| ChEMBL | Displacement of [3H]-5-HT from human 5-HT1A receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis | B | 8.58 | pKi | 2.65 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 1427-1430 [PMID:25759032] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in CHO-K1 cells incubated for 60 mins by liquid scintillation counting method | B | 8.58 | pKi | 2.65 | nM | Ki | Eur J Med Chem (2019) 183: 111690-111690 [PMID:31526973] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 cells | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (2008) 51: 5813-5822 [PMID:18800769] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HEK293 cells | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (2007) 50: 4214-4221 [PMID:17649988] |
| ChEMBL | Binding affinity against human 5-hydroxytryptamine 1A receptor | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Binding affinity against [3H]8-OH-DPAT-labeled 5-hydroxytryptamine 1A receptor sites in bovine hippocampus | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (1993) 36: 1069-1083 [PMID:8097538] |
| ChEMBL | Compound was evaluated for the binding affinity against [3H]8-OH-DPAT-labeled 5-hydroxytryptamine 1A receptor in bovine hippocampus | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (1993) 36: 1053-1068 [PMID:8097537] |
| ChEMBL | In vivo binding affinity towards [3H]8-OH-DPAT-labeled 5-hydroxytryptamine 1A receptor sites in bovine hippocampus. | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (1993) 36: 671-682 [PMID:8459396] |
| ChEMBL | Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand | B | 8.83 | pKi | 1.49 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1407-1412 [PMID:9871775] |
| ChEMBL | Binding affinity to 5HT1A receptor | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (2011) 54: 3086-3090 [PMID:21469694] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor expressed in CHO cells by liquid scintillation counting | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2010) 53: 1319-1328 [PMID:20041669] |
| ChEMBL | Binding affinity to 5HT1A receptor | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2010) 53: 1319-1328 [PMID:20041669] |
| ChEMBL | Binding affinity to 5-HT1A (unknown origin) | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127325-127325 [PMID:32631530] |
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 1A receptor was determined using [3H]8-OH-DPAT-as radioligand | B | 9.08 | pKi | 0.83 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 793-795 [PMID:11277522] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor stably expressed in CHO-K1 cell membranes measured after 60 mins by Microbeta2 scintillation counting method | B | 9.09 | pKi | 0.81 | nM | Ki | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from recombinant human 5HT1A receptor stably expressed in CHO-K1 cell membranes measured after 60 mins by microbeta2 scintillation counting method | B | 9.09 | pKi | 0.81 | nM | Ki | J Med Chem (2019) 62: 2750-2771 [PMID:30721053] |
| ChEMBL | Binding affinity to human 5HT1A receptor | B | 9.1 | pKi | 0.8 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127053-127053 [PMID:32107165] |
| ChEMBL | Displacement of [3H]-WAY100635 from human 5-HT1A receptor expresssed in stable CHO cell membrane incubated for 90 mins by microbeta counting method | B | 9.1 | pKi | 0.8 | nM | Ki | Bioorg Med Chem (2020) 28: 115578-115578 [PMID:32631561] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor | B | 9.1 | pKi | 0.79 | nM | Ki | J Med Chem (2008) 51: 2887-2890 [PMID:18433113] |
| ChEMBL | Displacement of [3H]8-OH-DAPT from human recombinant 5-HT1A receptor expressed in HEK cells measured after 60 to 90 mins by radioligand completion assay relative to control | B | 9.12 | pKi | 0.75 | nM | Ki | J Med Chem (2021) 64: 13510-13523 [PMID:34467758] |
| ChEMBL | Displacement of [3H]Way100635 from human recombinant 5-HT1A receptor expressed in CHO cell membranes by radioligand binding assay | B | 9.15 | pKi | 0.71 | nM | Ki | J Nat Prod (2015) 78: 722-729 [PMID:25695425] |
| ChEMBL | Displacement of radiolabeled 8OH-DPAT from human 5HT1A receptor | B | 9.18 | pKi | 0.66 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Binding affinity against [3H]- -8-OH-DPAT -labeled 5-hydroxytryptamine 1A sites in cloned CHO cells | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (1993) 36: 2208-2218 [PMID:8340922] |
| ChEMBL | Tested in vitro for the inhibition of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor, expressed in cloned CHO cells. | B | 9.4 | pKi | 0.4 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2759-2764 |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK-293 cells | B | 9.4 | pKi | 0.4 | nM | Ki | Eur J Med Chem (2015) 92: 221-235 [PMID:25557493] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human recombinant 5-HT1A receptor expressed in HEK293 cells | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2014) 57: 4543-4557 [PMID:24805037] |
| GtoPdb | - | - | 9.4 | pKi | 0.4 | nM | Ki |
J Pharmacol Exp Ther (1998) 284: 1082-94 [PMID:9495870]; Biochem Pharmacol (2003) 65: 435-40 [PMID:12527336]; Biosci Rep (2004) 24: 101-15 [PMID:15628665]; J Pharmacol Exp Ther (1997) 280: 1241-9 [PMID:9067310]; Synapse (2000) 35: 79-95 [PMID:10611634]; Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 205-17 [PMID:9550290]; Biochem J (1992) 285 ( Pt 3): 933-8 [PMID:1386736] |
| ChEMBL | Binding affinity to human 5-HT1A receptor by radioligand displacement assay | B | 9.68 | pKi | 0.21 | nM | Ki | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Displacement of [3H]OH-DPAT from human recombinant 5-HT1A receptor measured after 60 mins by scintillation counter method | B | 9.74 | pKi | 0.18 | nM | Ki | Eur J Med Chem (2019) 176: 292-309 [PMID:31112891] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor | B | 9.77 | pKi | 0.17 | nM | Ki | J Med Chem (2011) 54: 5320-5334 [PMID:21726069] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem (2013) 21: 7604-7611 [PMID:24262884] |
| ChEMBL | Displacement of radiolabeled 8OH-DPAT from human 5HT1A receptor | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Percent inhibition against 5-hydroxytryptamine 1A receptor at 1 uM | B | 9.18 | pIC50 | 0.66 | nM | IC50 | J Med Chem (2005) 48: 6887-6896 [PMID:16250647] |
| ChEMBL | Inhibition of human 5HT1A receptor | B | 9.23 | pIC50 | 0.59 | nM | IC50 | J Med Chem (2008) 51: 4150-4169 [PMID:18588282] |
| ChEMBL | Displacement of [3H]8-OHDPAT from human recombinant 5-HT1A receptor expressed in HEK293 cells | B | 9.28 | pIC50 | 0.53 | nM | IC50 | Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method | B | 9.28 | pIC50 | 0.53 | nM | IC50 | Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250] |
| ChEMBL | Binding affinity to human 5-HT1A receptor by radioligand displacement assay | B | 9.29 | pIC50 | 0.51 | nM | IC50 | Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449] |
| ChEMBL | Binding affinity to human 5-HT1A receptor by radioligand displacement assay | B | 9.48 | pIC50 | 0.33 | nM | IC50 | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Displacement of [3H]OH-DPAT from human recombinant 5-HT1A receptor measured after 60 mins by scintillation counter method | B | 9.55 | pIC50 | 0.28 | nM | IC50 | Eur J Med Chem (2019) 176: 292-309 [PMID:31112891] |
| ChEMBL | Agonist activity at human 5-HT1A receptor expressed in CHO cells after 90 mins by beta-arrestin-2 recruitment assay | B | 7.29 | pEC50 | 51.29 | nM | EC50 | Bioorg Med Chem (2015) 23: 4824-4830 [PMID:26081758] |
| ChEMBL | Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.49 | pEC50 | 32.36 | nM | EC50 | J Med Chem (2007) 50: 5024-5033 [PMID:17803293] |
| ChEMBL | Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay | F | 7.5 | pEC50 | 31.62 | nM | EC50 | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| ChEMBL | Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay | F | 7.5 | pEC50 | 31.62 | nM | EC50 | J Med Chem (2019) 62: 2750-2771 [PMID:30721053] |
| ChEMBL | Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding | F | 7.55 | pEC50 | 28.18 | nM | EC50 | J Med Chem (2007) 50: 865-876 [PMID:17300168] |
| ChEMBL | Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding | F | 7.59 | pEC50 | 26 | nM | EC50 | J Med Chem (2008) 51: 6980-7004 [PMID:18834188] |
| ChEMBL | Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay | F | 7.66 | pEC50 | 21.88 | nM | EC50 | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| ChEMBL | Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation | F | 7.82 | pEC50 | 15 | nM | EC50 | Eur J Med Chem (2013) 60: 42-50 [PMID:23279866] |
| ChEMBL | Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay | B | 7.84 | pEC50 | 14.45 | nM | EC50 | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| ChEMBL | Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay | B | 7.84 | pEC50 | 14.45 | nM | EC50 | J Med Chem (2019) 62: 2750-2771 [PMID:30721053] |
| ChEMBL | Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA | F | 7.92 | pEC50 | 12.02 | nM | EC50 | Bioorg Med Chem (2015) 23: 4824-4830 [PMID:26081758] |
| ChEMBL | In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells | F | 7.96 | pEC50 | 10.9 | nM | EC50 | J Med Chem (2005) 48: 3467-3470 [PMID:15887953] |
| ChEMBL | Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay | B | 8.09 | pEC50 | 8.13 | nM | EC50 | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| ChEMBL | Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay | B | 8.09 | pEC50 | 8.13 | nM | EC50 | J Med Chem (2019) 62: 2750-2771 [PMID:30721053] |
| ChEMBL | Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA | F | 8.1 | pEC50 | 8 | nM | EC50 | J Med Chem (2013) 56: 7851-7861 [PMID:24050112] |
| ChEMBL | Agonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assay | F | 8.22 | pEC50 | 6 | nM | EC50 | Bioorg Med Chem Lett (2019) 29: 126667-126667 [PMID:31547945] |
| ChEMBL | EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor | F | 8.24 | pEC50 | 5.82 | nM | EC50 | J Med Chem (2000) 43: 4701-4710 [PMID:11101361] |
| ChEMBL | Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay | F | 8.48 | pEC50 | 3.3 | nM | EC50 | Eur J Med Chem (2022) 229: 114045-114045 [PMID:34922191] |
| ChEMBL | In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor | F | 8.59 | pEC50 | 2.6 | nM | EC50 | J Med Chem (2005) 48: 3467-3470 [PMID:15887953] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Binding affinity against the site labelled by the 5-hydroxytryptamine 1A receptor agonist [3H]- 8-OH-DPAT | B | 8.6 | pKd | 2.5 | nM | Kd | J Med Chem (1994) 37: 4346-4351 [PMID:7996545] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor sites, in rat striatum membranes using [3H]- sandoz 205-501 as radioligand | B | 6.01 | pKi | 975 | nM | Ki | J Med Chem (1990) 33: 1541-1544 [PMID:2140413] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from rat cerebral cortex 5HT1A receptor measured after 15 mins by liquid scintillation counter method | B | 8.03 | pKi | 9.4 | nM | Ki | Bioorg Med Chem (2016) 24: 3994-4007 [PMID:27377863] |
| ChEMBL | In vitro binding affinity against 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT (agonist) as radioligand (sc) | B | 8.06 | pKi | 8.7 | nM | Ki | J Med Chem (1993) 36: 2059-2065 [PMID:8340910] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1A receptor in homogenated rat brain tissue, using by [3H]8-OH-DPAT as radioligand | B | 8.06 | pKi | 8.7 | nM | Ki | J Med Chem (1993) 36: 3409-3416 [PMID:8230131] |
| ChEMBL | Displacement of the radioligand [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor | B | 8.06 | pKi | 8.7 | nM | Ki | J Med Chem (1994) 37: 3263-3273 [PMID:7932553] |
| ChEMBL | Binding affinity was tested on 5-hydroxytryptamine 1A receptor using radioligand [3H]5-HT binding assay. | B | 8.37 | pKi | 4.3 | nM | Ki | J Med Chem (1996) 39: 4255-4260 [PMID:8863803] |
| ChEMBL | Displacement of [3H]5-HT from rat hippocampal 5-hydroxytryptamine 1A receptor with 10e-6 M ketanserin | B | 8.37 | pKi | 4.3 | nM | Ki | J Med Chem (1996) 39: 176-182 [PMID:8568804] |
| ChEMBL | Displacement of radioligand [3H]2-(di-N-propylamino)-8-hydroxytetralin from 5-hydroxytryptamine 1A receptor in rat frontal cortex homogenate | B | 8.55 | pKi | 2.8 | nM | Ki | J Med Chem (1993) 36: 2751-2760 [PMID:8410989] |
| 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 | 8.63 | pKi | 2.33 | nM | Ki | J Med Chem (1999) 42: 173-177 [PMID:9888842] |
| ChEMBL | The compound was evaluated for binding affinity against 5-hydroxytryptamine 1A receptor in rat hippocampal membranes using [3H]8-OH-DPAT as radioligand in the presence of 3*10e-5 M GTP gamma S | B | 8.65 | pKi | 2.26 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 2035-2038 |
| ChEMBL | Binding affinity of compound against 5-hydroxytryptamine 1A receptor binding site using radioligand [3H]8-OH-DPAT | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (1989) 32: 1959-1962 [PMID:2569041] |
| ChEMBL | Binding was determined on 5-hydroxytryptamine 1A receptor in rat hippocampal membranes | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (2001) 44: 4431-4442 [PMID:11728188] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor from rat hippocampal membranes | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (2002) 45: 5727-5735 [PMID:12477356] |
| ChEMBL | Binding affinity against the 5-hydroxytryptamine 1A receptor labelled with [3H]8-OH-DPAT in rat hippocampal homogenates | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (1998) 41: 4995-5001 [PMID:9836617] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor of rat cortex membranes | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2003) 46: 3555-3558 [PMID:12877594] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1A receptor by displacing [3H]8-OH-DPAT radioligand in rat cortex membrane | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2002) 45: 3603-3611 [PMID:12166933] |
| ChEMBL | Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand. | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor in rat cerebral cortex | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 171-173 [PMID:12482417] |
| ChEMBL | Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement | B | 8.73 | pKi | 1.86 | nM | Ki | J Med Chem (1996) 39: 126-134 [PMID:8568799] |
| ChEMBL | Binding affinity for 5-hydroxytryptamine 1A receptor with [3H]5-HT | B | 8.8 | pKi | 1.59 | nM | Ki | J Med Chem (1994) 37: 105-112 [PMID:8289183] |
| ChEMBL | Inhibitory affinity constant against 5-hydroxytryptamine 1A receptor | B | 8.84 | pKi | 1.44 | nM | Ki | J Med Chem (1995) 38: 1701-1710 [PMID:7752194] |
| ChEMBL | In vitro ability to displace [3H]8-hydroxy-2-(di-n-propylamino) tetralin binding from 5-hydroxytryptamine 1A receptor site. | B | 8.84 | pKi | 1.44 | nM | Ki | J Med Chem (1992) 35: 2369-2374 [PMID:1535661] |
| ChEMBL | Binding affinity for rat cortex 5-hydroxytryptamine 1A receptor, by displacement of 0.2 nM [3H]8-OH-DPAT radioligand | B | 8.85 | pKi | 1.41 | nM | Ki | J Med Chem (1998) 41: 5070-5083 [PMID:9836623] |
| ChEMBL | Binding affinity to 5HT1A receptor in rat cortex membrane | B | 8.85 | pKi | 1.41 | nM | Ki | J Med Chem (2007) 50: 5024-5033 [PMID:17803293] |
| ChEMBL | Displacement of [3H]OH-DPAT from rat cortex 5HT1A receptor | B | 8.85 | pKi | 1.41 | nM | Ki | J Med Chem (2007) 50: 865-876 [PMID:17300168] |
| ChEMBL | In vitro by displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor on rat cortical membrane | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (1997) 40: 586-593 [PMID:9046349] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5-HT1A receptor in Wistar rat cerebral hippocampus membrane after 10 mins | B | 8.92 | pKi | 1.2 | nM | Ki | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Binding affinity to the rat 5-hydroxytryptamine 1A receptor | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2003) 46: 646-649 [PMID:12570387] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from 5-HT1A receptor in rat hippocampal membranes | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2017) 60: 2605-2628 [PMID:28244748] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor in Wistar Han rat hippocampal membranes | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2004) 47: 6616-6624 [PMID:15588097] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (1988) 31: 867-870 [PMID:2965244] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor of rat hippocampus mambranes | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
| ChEMBL | Binding affinity at [3H]8-OH-DPAT-Labeled 5-hydroxytryptamine 1A receptor sites in rat brain hippocampal membranes | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (1989) 32: 253-256 [PMID:2521252] |
| ChEMBL | In vitro ability to displace [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor sites of rat brain cortex. | B | 8.93 | pKi | 1.18 | nM | Ki | J Med Chem (1995) 38: 1273-1277 [PMID:7731013] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from rat hippocampal 5-hydroxytryptamine 1A receptor | B | 8.96 | pKi | 1.09 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 2035-2038 |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from 5-HT1A receptor in Sprague-Dawley rat cerebral cortex after 15 mins | B | 8.99 | pKi | 1.02 | nM | Ki | J Med Chem (2013) 56: 7851-7861 [PMID:24050112] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor sites in cortical membranes using [3H]8-OH-DPAT as radioligand | B | 9 | pKi | 1 | nM | Ki | J Med Chem (1990) 33: 1541-1544 [PMID:2140413] |
| ChEMBL | Affinity for 5-hydroxytryptamine 1A receptor site | B | 9 | pKi | 1 | nM | Ki | J Med Chem (1989) 32: 2311-2318 [PMID:2795604] |
| ChEMBL | Displacement of [3H]8OH-DPAT from 5HT1A in Sprague-Dawley rat brain cortex by liquid scintillation counting | B | 9.1 | pKi | 0.8 | nM | Ki | Eur J Med Chem (2010) 45: 752-759 [PMID:19954866] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from Sprague-Dawley rat brain cortex serotonin 5-HT1A receptor after 30 mins by liquid scintillation counting | B | 9.1 | pKi | 0.8 | nM | Ki | Eur J Med Chem (2012) 47: 520-529 [PMID:22133459] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat cortex membrane | B | 9.19 | pKi | 0.64 | nM | Ki | Bioorg Med Chem (2007) 15: 7581-7589 [PMID:17900912] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor by the displacement of [3H]8-OH-DPAT in membrane homogenates of hippocampal tissue of rat brain | B | 9.2 | pKi | 0.63 | nM | Ki | J Med Chem (1993) 36: 3161-3165 [PMID:8230102] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from rat hippocampal 5-hydroxytryptamine 1A receptor | B | 9.27 | pKi | 0.54 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 2035-2038 |
| ChEMBL | In vitro displacement of radioactively labeled ligand [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor site in CHO cells | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (1995) 38: 725-734 [PMID:7861420] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor of rat hippocampal membranes | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Binding affinity against rat 5-hydroxytryptamine 1A receptor | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1A receptor from CHO-K1 cells, using [3H]8-OH-DPAT as the radioligand. | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (1995) 38: 2202-2216 [PMID:7783152] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from rat striata 5-hydroxytryptamine 1A receptor | B | 9.33 | pKi | 0.47 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 509-512 [PMID:10743959] |
| ChEMBL | The compound was evaluated for binding affinity against 5-hydroxytryptamine 1A receptor in rat hippocampal membranes using [3H]8-OH-DPAT as radioligand in the presence of 1 mM of MnCl2 | B | 9.57 | pKi | 0.27 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 2035-2038 |
| ChEMBL | Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus | F | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor using receptor binding assay | B | 8.09 | pIC50 | 8.06 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 2857-2862 |
| ChEMBL | In vitro binding activity against 5-hydroxytryptamine 1A receptor from homogenized rat brain, using [3H]8-OH-DPAT as the radioligand | B | 8.35 | pIC50 | 4.46 | nM | IC50 | J Med Chem (1989) 32: 2273-2276 [PMID:2571729] |
| ChEMBL | The compound was tested in vitro for inhibitory activity against 5-HT1A receptor in rats, using [3H]8-OH-DPAT as radioligand | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (1992) 35: 3984-3990 [PMID:1433207] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand. | B | 8.52 | pIC50 | 3.02 | nM | IC50 | J Med Chem (1988) 31: 1087-1093 [PMID:3373482] |
| ChEMBL |
Concentration necessary to achieve half maximal inhibition of [3H]8-Hydroxy-2-(di-n-propylamino)tetralin binding to 5-hydroxytryptamine 1A receptor at 1 uM |
B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1989) 32: 720-727 [PMID:2537429] |
| ChEMBL | Binding affinity to 5-hydroxytryptamine 1A receptor in rat hippocampus membranes,3H-8-OH-DPAT and buspirone for nonspecific binding (NSB) | B | 8.62 | pIC50 | 2.4 | nM | IC50 | J Med Chem (1996) 39: 4285-4298 [PMID:8863806] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1A (5-HT1A) receptor in rat hippocampus membranes | B | 8.62 | pIC50 | 2.4 | nM | IC50 | J Med Chem (1994) 37: 1779-1793 [PMID:7912735] |
| ChEMBL | Binding affinity towards rat 5-hydroxytryptamine 1A receptor was evaluated using [3H]8-OH-DPAT as radioligand | B | 8.68 | pIC50 | 2.1 | nM | IC50 | J Med Chem (1996) 39: 4928-4934 [PMID:8960552] |
| ChEMBL | Binding affinity against serotonin 5-hydroxytryptamine 1A receptor in rat hippocampus membrane using [3H]8-OH-DPAT as radioligand | B | 8.68 | pIC50 | 2.1 | nM | IC50 | J Med Chem (1996) 39: 3195-3202 [PMID:8759642] |
| ChEMBL | In vitro ability to inhibit binding of radioligand [3H]8-OH-DPAT to 5-hydroxytryptamine 1A receptor in rat cerebral cortex | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (1994) 37: 99-104 [PMID:8289207] |
| ChEMBL | In vitro binding affinity measured on serotonin 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand. | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (1995) 38: 942-949 [PMID:7699710] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand. | B | 6.2 | pKi | 638 | nM | Ki | J Med Chem (1995) 38: 2202-2216 [PMID:7783152] |
| ChEMBL | Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand | B | 6.25 | pKi | 559 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1407-1412 [PMID:9871775] |
| GtoPdb | - | - | 6.2 | pIC50 | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (1997) 356: 328-34 [PMID:9303569] |
| ChEMBL | The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line | F | 6.59 | pEC50 | 260 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 1407-1412 [PMID:9871775] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
| ChEMBL | Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand. | B | 4.2 | pKi | 63000 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| ChEMBL | Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1988) 31: 867-870 [PMID:2965244] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 2035-2038 |
| ChEMBL | Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor | B | 5.59 | pKi | 2570 | nM | Ki | J Med Chem (1994) 37: 105-112 [PMID:8289183] |
| ChEMBL | Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand | B | 5.42 | pIC50 | 3801.89 | nM | IC50 | J Med Chem (1988) 31: 1087-1093 [PMID:3373482] |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1D receptor alpha expressed in CHO-K1 cells, using [3H]-5-HT as the radioligand. | B | 6.79 | pKi | 164 | nM | Ki | J Med Chem (1995) 38: 2202-2216 [PMID:7783152] |
| ChEMBL | Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1D receptor using [3H]-5-CT as radioligand | B | 6.94 | pKi | 115 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1407-1412 [PMID:9871775] |
| GtoPdb | - | - | 7.3 | pKi | - | - | - |
Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663]; Naunyn Schmiedebergs Arch Pharmacol (1997) 356: 328-34 [PMID:9303569]; Mol Pharmacol (1996) 50: 1567-80 [PMID:8967979] |
| 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| GtoPdb | - | - | 5.6 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| Serotonin 2a (5-HT2a) receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 2 receptor | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortex | B | 4.31 | pIC50 | 49000 | nM | IC50 | J Med Chem (1994) 37: 1779-1793 [PMID:7912735] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| ChEMBL | The binding affinity was evaluated on 5-hydroxytryptamine 2A receptor expressed in rat cortex by using [3H]ketanserin as radioligand. | B | 6 | pKi | <6 | nM | Log Ki | J Med Chem (1999) 42: 2961-2968 [PMID:10425105] |
| ChEMBL | Binding affinity towards rat 5-hydroxytryptamine 2A receptor was evaluated using [3H]- ketanserin as radioligand | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1996) 39: 4928-4934 [PMID:8960552] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 2A receptor by displacement of [3H]-ketanserin from rat prefrontal cerebral cortex mambranes | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Inhibition of [3H]mesulergine binding to 5-hydroxytryptamine 1C receptor of pig choroid Plexus | B | 4.83 | pKi | 14800 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Evaluated for the binding affinity to porcine choroid plexus at 5-hydroxytryptamine 2C receptor binding site by using [3H]-MES as a radioligand. | B | 5.14 | pKi | 7250 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| GtoPdb | - | - | 5.6 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| 5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16] | ||||||||
| ChEMBL | Ability to displace [3H]granisetron specifically bound to 5-hydroxytryptamine 3 receptor in rat cortical membrane | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (1998) 41: 728-741 [PMID:9513601] |
| 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 5A receptor | B | 5.6 | pKi | 2500 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand | B | 5.6 | pKi | 2500 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| GtoPdb | - | - | 5.7 | pKi | - | - | - |
FEBS Lett (1994) 355: 242-6 [PMID:7988681]; Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685] |
| ChEMBL | Binding affinity for rodent 5-hydroxytryptamine 5A receptor | B | 6 | pKi | 1000 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| 5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966] | ||||||||
| GtoPdb | - | - | 5.9 | pKi | - | - | - |
Mol Pharmacol (1993) 43: 313-9 [PMID:8450829]; Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells | B | 6.3 | pKi | 501.19 | nM | Ki | Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003] |
| ChEMBL | Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor | B | 6.33 | pKi | 466 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis | B | 6.41 | pKi | 388 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 1427-1430 [PMID:25759032] |
| ChEMBL | Displacement of [3H]-5-HT from recombinant human 5-HT7A receptor expressed in CHOK1 cell membranes after 40 mins by liquid scintillation counting method | B | 6.41 | pKi | 388 | nM | Ki | Bioorg Med Chem (2017) 25: 1250-1259 [PMID:28063784] |
| ChEMBL | Displacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry | B | 6.41 | pKi | 388 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 4052-4056 [PMID:27396505] |
| GtoPdb | - | - | 7.6 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2001) 363: 620-32 [PMID:11414657]; Br J Pharmacol (1997) 122: 126-32 [PMID:9298538]; J Biol Chem (1993) 268: 23422-6 [PMID:8226867]; Br J Pharmacol (1998) 124: 1300-6 [PMID:9720804] |
| 5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304] | ||||||||
| GtoPdb | - | - | 6.6 | pKi | - | - | - | Mol Pharmacol (1993) 44: 229-36 [PMID:8394987] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
| ChEMBL | Binding affinity towards rat 5-hydroxytryptamine 7 receptor | B | 6.82 | pKi | 150 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| GtoPdb | - | - | 7.5 | pKi | - | - | - |
J Biol Chem (1993) 268: 18200-4 [PMID:8394362]; Proc Natl Acad Sci USA (1993) 90: 8547-51 [PMID:8397408] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Binding affinity against serotonin transporter (SERT) by displacement of [3H]paroxetine in male wistar rats | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | Binding affinity against sigma receptor | B | 5.61 | pKi | >2427 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] | ||||||||
| ChEMBL | Inhibition of [3H]DTG binding to sigma receptor in rat hippocampus | B | 5.28 | pKi | 5240 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| GtoPdb | - | - | 5.5 | pKi | - | - | - |
Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]; Eur J Pharmacol (2004) 484: 127-39 [PMID:14744596] |
| 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939] | ||||||||
| GtoPdb | - | - | 5.8 | pKi | - | - | - | Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639] |
| 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| GtoPdb | - | - | 5.4 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994] | ||||||||
| GtoPdb | - | - | 5.4 | pKi | - | - | - | Mol Pharmacol (1993) 43: 419-26 [PMID:8450835] |
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]
