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];
Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
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];
Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
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];
Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]