BMY-7378 [Ligand Id: 9] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL13647 (BMY-7378)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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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 Affinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptor B 6.42 pKd 380.19 nM Kd J. Med. Chem. (2002) 45: 1633-1643 [PMID:11931617]
ChEMBL Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement. B 6.36 pKi 436.52 nM Ki J. Med. Chem. (1998) 41: 4844-4853 [PMID:9822553]
ChEMBL Displacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method B 6.41 pKi 389.05 nM Ki Eur J Med Chem (2017) 125: 435-452 [PMID:27689727]
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 6.42 pKi 380.19 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 6.42 pKi 380.19 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 2017-2020 [PMID:20185311]
ChEMBL Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique B 6.42 pKi 380.19 nM Ki Eur. J. Med. Chem. (2010) 45: 3740-3751 [PMID:20605276]
ChEMBL Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting B 6.42 pKi 380.19 nM Ki J. Med. Chem. (2012) 55: 23-36 [PMID:22145629]
ChEMBL Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins B 6.42 pKi 380.19 nM Ki J. Med. Chem. (2013) 56: 584-588 [PMID:23252794]
ChEMBL Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor B 6.42 pKi 380.19 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 6.42 pKi 380.19 nM Ki J. Med. Chem. (2008) 51: 6359-6370 [PMID:18817363]
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 (n >= 2) B 6.53 pKi 294 nM Ki J. Med. Chem. (1998) 41: 1205-1208 [PMID:9548811]
ChEMBL Binding affinity for human Alpha-1A adrenergic receptor B 6.54 pKi 290 nM Ki J. Med. Chem. (2005) 48: 3076-3079 [PMID:15828846]
ChEMBL In vitro binding affinity at human Alpha-1A adrenergic receptor. B 6.6 pKi 251 nM Ki J. Med. Chem. (2003) 46: 2877-2894 [PMID:12825930]
ChEMBL Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive B 6.6 pKi 250 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 657-664 [PMID:15664832]
ChEMBL Binding affinity for human Alpha-1A adrenergic receptor B 6.89 pKi 130 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
GtoPdb - - 7 pKi - - - Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121];
Bioorg Med Chem Lett (2001) 11: 1119-21 [PMID:11354357]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Binding affinity towards bovine Alpha-1A adrenergic receptor B 7.37 pKi 43 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL In vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferens B 5.98 pKd 1047.13 nM Kd Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
ChEMBL Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens. F 6.94 pKd 114.82 nM Kd J. Med. Chem. (1998) 41: 4844-4853 [PMID:9822553]
ChEMBL Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor F 7.01 pKd 97.72 nM Kd J. Med. Chem. (2002) 45: 1633-1643 [PMID:11931617]
ChEMBL Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor B 6.21 pKi 620 nM Ki J. Med. Chem. (1998) 41: 1205-1208 [PMID:9548811]
ChEMBL In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens. B 6.31 pKi 494.7 nM Ki J. Med. Chem. (2004) 47: 1900-1918 [PMID:15055991]
ChEMBL Binding affinity towards rat Alpha-1A adrenergic receptor B 6.95 pKi 112 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
GtoPdb - - 7 pKi - - - Bioorg Med Chem Lett (2001) 11: 1119-21 [PMID:11354357]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Displacement of [3H]prazosin from human cloned Alpha-1B adrenoceptor expressed in CHO cells B 6.15 pKi 707.95 nM Ki J. Med. Chem. (2008) 51: 6359-6370 [PMID:18817363]
ChEMBL Displacement [3H]prazosin of human recombinant Alpha-1B adrenergic receptor expressed in CHO cells by rapid filtration technique B 6.15 pKi 707.95 nM Ki Eur. J. Med. Chem. (2010) 45: 3740-3751 [PMID:20605276]
ChEMBL Displacement of [3H]prazosin from recombinant human alpha1b adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method B 6.15 pKi 707.95 nM Ki Eur J Med Chem (2017) 125: 435-452 [PMID:27689727]
ChEMBL Displacement of [3H]prazosin from human recombinant alpha1B adrenergic receptor expressed in CHO cell membranes after 30 mins B 6.15 pKi 707.95 nM Ki J. Med. Chem. (2013) 56: 584-588 [PMID:23252794]
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 6.15 pKi 707.95 nM Ki Eur J Med Chem (2019) 168: 461-473 [PMID:30844609]
ChEMBL Displacement of [3H]prazosin from human Alpha-1B adrenergic receptor expressed in CHO cells B 6.15 pKi 707.95 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 2017-2020 [PMID:20185311]
ChEMBL Affinity constant on CHO cells expressing Human recombinant Alpha-1B adrenergic receptor B 6.15 pKi 707.95 nM Ki J. Med. Chem. (2002) 45: 1633-1643 [PMID:11931617]
ChEMBL Displacement of [3H]prazosin from human recombinant alpha1B adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting B 6.15 pKi 707.95 nM Ki J. Med. Chem. (2012) 55: 23-36 [PMID:22145629]
ChEMBL In vitro binding affinity at human Alpha-1B adrenergic receptor. B 6.2 pKi 631 nM Ki J. Med. Chem. (2003) 46: 2877-2894 [PMID:12825930]
ChEMBL Binding affinity for human Alpha-1B adrenergic receptor B 6.72 pKi 191 nM Ki J. Med. Chem. (2005) 48: 3076-3079 [PMID:15828846]
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 (n >= 2) B 6.72 pKi 191 nM Ki J. Med. Chem. (1998) 41: 1205-1208 [PMID:9548811]
ChEMBL Binding affinity constant against alpha-1B adrenergic receptor of guinea pig spleen B 6.77 pKi 168.2 nM Ki J. Med. Chem. (2004) 47: 1900-1918 [PMID:15055991]
ChEMBL Binding affinity towards human Alpha-1B adrenergic receptor B 7.03 pKi 94.3 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
ChEMBL Displacement of [3H]prazosin from human cloned Alpha-1B adrenergic receptor B 7.16 pKi 69.18 nM Ki J. Med. Chem. (1999) 42: 4214-4224 [PMID:10514291]
ChEMBL Binding affinity at human cloned Alpha-1B adrenergic receptor in chinese hamster ovary cells by [3H]prazosin displacement. B 7.19 pKi 64.57 nM Ki J. Med. Chem. (1998) 41: 4844-4853 [PMID:9822553]
GtoPdb - - 7.5 pKi - - - Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121];
Bioorg Med Chem Lett (2001) 11: 1119-21 [PMID:11354357]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL In vitro functional activity at Alpha-1B adrenergic receptor in rat spleen F 7.37 pKd 42.66 nM Kd Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
ChEMBL Antagonistic affinity tested against isolated Rat Spleen Alpha-1B adrenergic receptor F 7.48 pKd 33.11 nM Kd J. Med. Chem. (2002) 45: 1633-1643 [PMID:11931617]
ChEMBL Antagonism of phenylephrine stimulated contraction of the rat isolated spleen. F 7.55 pKd 28.18 nM Kd J. Med. Chem. (1998) 41: 4844-4853 [PMID:9822553]
ChEMBL Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1B adrenergic receptor B 6.48 pKi 328 nM Ki J. Med. Chem. (1998) 41: 1205-1208 [PMID:9548811]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL In vitro binding affinity at human Alpha-1D adrenergic receptor. B 8.2 pKi 6.3 nM Ki J. Med. Chem. (2003) 46: 2877-2894 [PMID:12825930]
ChEMBL Binding affinity for human Alpha-1D adrenergic receptor B 8.8 pKi 1.6 nM Ki J. Med. Chem. (2005) 48: 3076-3079 [PMID:15828846]
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 (n >= 2) B 8.8 pKi 1.6 nM Ki J. Med. Chem. (1998) 41: 1205-1208 [PMID:9548811]
ChEMBL Displacement of [3H]prazosin from human cloned Alpha-1D adrenergic receptor B 8.84 pKi 1.45 nM Ki J. Med. Chem. (1999) 42: 4214-4224 [PMID:10514291]
ChEMBL Displacement of [3H]prazosin from human Alpha-1D adrenergic receptor expressed in CHO cells B 8.89 pKi 1.29 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 2017-2020 [PMID:20185311]
ChEMBL Displacement [3H]prazosin of human recombinant Alpha-1D adrenergic receptor expressed in CHO cells by rapid filtration technique B 8.89 pKi 1.29 nM Ki Eur. J. Med. Chem. (2010) 45: 3740-3751 [PMID:20605276]
ChEMBL Displacement of [3H]prazosin from human recombinant Alpha-1D adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting B 8.89 pKi 1.29 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 8.89 pKi 1.29 nM Ki J. Med. Chem. (2013) 56: 584-588 [PMID:23252794]
ChEMBL Displacement of [3H]prazosin from recombinant human alpha1d adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method B 8.89 pKi 1.29 nM Ki Eur J Med Chem (2017) 125: 435-452 [PMID:27689727]
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 8.89 pKi 1.29 nM Ki Eur J Med Chem (2019) 168: 461-473 [PMID:30844609]
ChEMBL Binding affinity at human cloned Alpha-1D adrenergic receptor in chinese hamster ovary cells by [3H]prazosin displacement. B 8.89 pKi 1.29 nM Ki J. Med. Chem. (1998) 41: 4844-4853 [PMID:9822553]
ChEMBL Affinity constant on CHO cells expressing Human recombinant Alpha-1D adrenergic receptor B 8.89 pKi 1.29 nM Ki J. Med. Chem. (2002) 45: 1633-1643 [PMID:11931617]
ChEMBL Displacement of [3H]prazosin from human cloned alpha1D adrenoceptor expressed in CHO cells B 8.89 pKi 1.29 nM Ki J. Med. Chem. (2008) 51: 6359-6370 [PMID:18817363]
GtoPdb - - 9.1 pKi - - - Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121];
Bioorg Med Chem Lett (2001) 11: 1119-21 [PMID:11354357]
ChEMBL Binding affinity towards human Alpha-1D adrenergic receptor B 9.11 pKi 0.78 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
ChEMBL In vitro functional activity at Alpha-1D adrenergic receptor in rat aorta B 8.22 pKd 6.03 nM Kd Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
ChEMBL Antagonism of norepinephrine induced contraction of rat isolated thoracic aorta. F 8.34 pKd 4.57 nM Kd J. Med. Chem. (1998) 41: 4844-4853 [PMID:9822553]
ChEMBL Antagonistic affinity tested against isolated Rat Thoracic Aorta Alpha-1D adrenergic receptor F 8.4 pKd 3.98 nM Kd J. Med. Chem. (2002) 45: 1633-1643 [PMID:11931617]
ChEMBL Antagonist activity at adrenergic alpha 1D receptor in rat thoracic aorta assessed as inhibition of noradrenaline-induced contraction after 1 hr F 8.52 pKd 3.02 nM Kd Eur. J. Med. Chem. (2011) 46: 3000-3012 [PMID:21549456]
ChEMBL Binding affinity to the adrenergic receptor alpha-1D of rat aorta B 8.07 pKi 8.6 nM Ki J. Med. Chem. (2004) 47: 1900-1918 [PMID:15055991]
ChEMBL Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1D adrenergic receptor B 8.62 pKi 2.4 nM Ki J. Med. Chem. (1998) 41: 1205-1208 [PMID:9548811]
GtoPdb - - 9 pKi - - - Bioorg Med Chem Lett (2001) 11: 1119-21 [PMID:11354357]
ChEMBL Binding affinity towards rat Alpha-1D adrenergic receptor B 9.02 pKi 0.96 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Binding affinity for human Dopamine receptor D2 B 7.85 pKi 14 nM Ki J. Med. Chem. (2005) 48: 3076-3079 [PMID:15828846]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Displacement of [3H]spiperone from rat brain Dopamine receptor D2 B 7.31 pKi 48.98 nM Ki J. Med. Chem. (1999) 42: 4214-4224 [PMID:10514291]
ChEMBL Binding affinity at native Dopamine receptor D2 in rat striatum by [3H]spiperone displacement. B 7.32 pKi 47.86 nM Ki J. Med. Chem. (1998) 41: 4844-4853 [PMID:9822553]
ChEMBL In vitro binding affinity towards Dopamine receptor D2 in rat striatum was determined using [3H]-spiperone as radioligand B 7.76 pKi 17.38 nM Ki J. Med. Chem. (1995) 38: 4044-4055 [PMID:7562940]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL Binding affinity for rat Dopamine receptor D3 B 8.51 pKi 3.1 nM Ki J. Med. Chem. (2005) 48: 3076-3079 [PMID:15828846]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity at human cloned 5-hydroxytryptamine 1A receptor expressed in HeLa cells by [3H]8-hydroxy-2-(di-n-propylamino)tetraline displacement. B 8.76 pKi 1.74 nM Ki J. Med. Chem. (1998) 41: 4844-4853 [PMID:9822553]
ChEMBL Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor expressed in human HeLa cells B 8.9 pKi 1.26 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 2017-2020 [PMID:20185311]
ChEMBL Displacement of [3H]8-OH-DPAT from recombinant human 5-HT1A receptor expressed in HeLa cell membranes after 30 mins by TopCount liquid scintillation counting method B 8.9 pKi 1.26 nM Ki Eur J Med Chem (2017) 125: 435-452 [PMID:27689727]
ChEMBL Displacement of [3H]-OH-DPAT from human recombinant 5HT1A receptor expressed in HeLa cells after 30 mins by liquid scintillation counting B 8.9 pKi 1.26 nM Ki J. Med. Chem. (2012) 55: 23-36 [PMID:22145629]
ChEMBL Inhibitory constant value against the 5-hydroxytryptamine 1A receptor B 8.9 pKi 1.26 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 1185-1188 [PMID:15686938]
ChEMBL Displacement [3H]8-OH-DPAT of human cloned 5HT1A receptor expressed in human HeLa cells by rapid filtration technique B 8.9 pKi 1.26 nM Ki Eur. J. Med. Chem. (2010) 45: 3740-3751 [PMID:20605276]
ChEMBL Displacement of [3H]8-hydroxy-2-(di-n-propylamino)tetralin from human 5-hydroxytryptamine 1A receptor B 9.03 pKi 0.93 nM Ki J. Med. Chem. (1999) 42: 4214-4224 [PMID:10514291]
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 9.1 pKi 0.8 nM Ki J. Med. Chem. (2004) 47: 1900-1918 [PMID:15055991]
ChEMBL Binding affinity for human 5-hydroxytryptamine 1A receptor B 9.34 pKi 0.46 nM Ki J. Med. Chem. (2005) 48: 3076-3079 [PMID:15828846]
ChEMBL Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in human HeLa cells B 9.43 pKi 0.37 nM Ki J. Med. Chem. (2008) 51: 6359-6370 [PMID:18817363]
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 9.43 pKi 0.37 nM Ki Eur J Med Chem (2017) 125: 233-244 [PMID:27662034]
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 9.43 pKi 0.37 nM Ki Eur J Med Chem (2019) 168: 461-473 [PMID:30844609]
ChEMBL Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HeLa cell membranes after 30 mins B 9.43 pKi 0.37 nM Ki J. Med. Chem. (2013) 56: 584-588 [PMID:23252794]
ChEMBL Affinity constant on CHO cells expressing Human recombinant 5-hydroxytryptamine receptor 1A B 9.43 pKi 0.37 nM Ki J. Med. Chem. (2002) 45: 1633-1643 [PMID:11931617]
GtoPdb - - 8 pIC50 - - - Life Sci (1997) 60: 653-65 [PMID:9048968]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement B 7.1 pKi 79.43 nM Ki J. Med. Chem. (1996) 39: 126-134 [PMID:8568799]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor in the rat brain (hippocampus) using [3H]8-OH-DPAT B 8.09 pKi 8.2 nM Ki J. Med. Chem. (1996) 39: 1125-1129 [PMID:8676348]
ChEMBL Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement B 8.62 pKi 2.4 nM Ki J. Med. Chem. (1996) 39: 126-134 [PMID:8568799]
ChEMBL Binding affinity at 5-hydroxytryptamine 1A receptor B 8.71 pKi 1.95 nM Ki J. Med. Chem. (1995) 38: 4044-4055 [PMID:7562940]
ChEMBL Compound was evaluated for its ability to displace [3H]8-OH-DPAT from serotonin 5-hydroxytryptamine 1A receptor in rat cerebral cortex membranes B 8.62 pIC50 2.4 nM IC50 Bioorg. Med. Chem. Lett. (1996) 6: 689-694
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL Binding affinity at 5-hydroxytryptamine 1B receptor B 5 pKi >10000 nM Ki J. Med. Chem. (1995) 38: 4044-4055 [PMID:7562940]

ChEMBL data shown on this page come from version 28:

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