WB 4101 [Ligand Id: 499] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL25554 (WB-4101)
  • 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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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • 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-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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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 Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor B 9.37 pKi 0.43 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 9.37 pKi 0.43 nM Ki J. Med. Chem. (2008) 51: 6359-6370 [PMID:18817363]
ChEMBL Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells B 9.37 pKi 0.43 nM Ki Bioorg. Med. Chem. (2010) 18: 7065-7077 [PMID:20801662]
ChEMBL Binding affinity to adrenergic alpha1A receptor (unknown origin) B 9.37 pKi 0.43 nM Ki Med Chem Res (2011) 20: 1455-1464
ChEMBL Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins B 9.37 pKi 0.43 nM Ki J. Med. Chem. (2013) 56: 584-588 [PMID:23252794]
ChEMBL Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay B 9.37 pKi 0.43 nM Ki J. Med. Chem. (2003) 46: 1504-1511 [PMID:12672251]
ChEMBL Antagonistic affinity tested against isolated Human recombinant Thoracic Aorta Alpha-1A adrenergic receptor F 9.37 pKi 0.43 nM Ki J. Med. Chem. (2002) 45: 1633-1643 [PMID:11931617]
ChEMBL Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi B 9.37 pKi 0.43 nM Ki J. Med. Chem. (2003) 46: 4895-4903 [PMID:14584940]
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 9.37 pKi 9.37 nM Log Ki J. Med. Chem. (1999) 42: 2961-2968 [PMID:10425105]
ChEMBL Binding affinity to adrenergic alpha1A receptor (unknown origin) B 9.37 pKi 0.43 nM Ki Med Chem Res (2011) 20: 1455-1464
ChEMBL Binding affinity against Alpha-1A adrenergic receptor from human clone B 9.43 pKi 0.37 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Displacement of [3H]prazosin from human recombinant adrenergic alpha-1A receptor expressed in CHO cell membranes incubated for 60 mins B 9.8 pKi 0.16 nM Ki J Med Chem (2020) 63: 433-439 [PMID:31834797]
ChEMBL Binding affinity was tested on human Alpha-1A adrenergic receptor B 9.8 pKi 0.16 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
GtoPdb - - 9.8 pKi - - - Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248];
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358];
FEBS Lett (1998) 422: 279-83 [PMID:9490024];
Eur J Pharmacol (1999) 370: 337-43 [PMID:10334511]
ChEMBL Antagonist activity at human recombinant alpha1A adrenoceptor assessed as inhibition of epinephrine-induced intracellular Ca2+ release B 9 pIC50 1 nM IC50 J. Med. Chem. (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL Antagonist activity against human recombinant alpha1 receptor expressed in CHOK1 cells assessed as reduction in epinephrine-induced increase in intracellular Ca2+ levels B 9 pIC50 1 nM IC50 Eur. J. Med. Chem. (2015) 92: 221-235 [PMID:25557493]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand B 9.21 pKi 0.62 nM Ki J. Med. Chem. (1996) 39: 2253-2258 [PMID:8667368]
ChEMBL Binding affinity of compound towards Alpha-1 adrenergic receptor using [3H]prazosin 0.5 nM ligand in frontal cortex calf was determined B 9.22 pKi 0.6 nM Ki J. Med. Chem. (1997) 40: 952-960 [PMID:9083484]
ChEMBL Binding affinity against Alpha-1A adrenergic receptor from bovine clone B 9.46 pKi 0.35 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate F 9.18 pKd 0.66 nM Kd J. Med. Chem. (2006) 49: 7140-7149 [PMID:17125266]
ChEMBL Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor F 9.27 pKd 0.54 nM Kd J. Med. Chem. (2002) 45: 1633-1643 [PMID:11931617]
ChEMBL Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (Alpha-1A adrenergic receptor ) F 9.36 pKd 0.44 nM Kd J. Med. Chem. (2003) 46: 1504-1511 [PMID:12672251]
ChEMBL Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens F 9.36 pKd 0.44 nM Kd J. Med. Chem. (2006) 49: 7140-7149 [PMID:17125266]
ChEMBL Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor F 9.51 pKd 0.31 nM Kd J. Med. Chem. (2002) 45: 1633-1643 [PMID:11931617]
ChEMBL Antagonistic activity at ADRA1A in isolated rat prostatic vas deferens F 9.51 pKd 0.31 nM Kd Bioorg. Med. Chem. Lett. (2006) 16: 150-153 [PMID:16216506]
ChEMBL Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand B 8.89 pKi 1.29 nM Ki J. Med. Chem. (1996) 39: 2253-2258 [PMID:8667368]
ChEMBL Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland B 10.1 pKi 0.08 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
GtoPdb - - 10.2 pKi - - - J Biol Chem (2001) 276: 25366-71 [PMID:11331292]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Binding affinity towards Alpha-1B adrenergic receptor cloned receptor hamster smooth muscle using [3H]prazosin as radioligand B 7.24 pKi 57.34 nM Ki J. Med. Chem. (1996) 39: 2253-2258 [PMID:8667368]
ChEMBL Binding affinity against Alpha-1B adrenergic receptor from hamster clones. B 7.43 pKi 37 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
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 8 pKi 8 nM Log Ki J. Med. Chem. (1999) 42: 2961-2968 [PMID:10425105]
ChEMBL Displacement of [3H]prazosin from human cloned Alpha-1B adrenergic receptor B 8 pKi 10 nM Ki J. Med. Chem. (1999) 42: 4214-4224 [PMID:10514291]
ChEMBL Displacement of [3H]prazosin from human cloned Alpha-1B adrenoceptor expressed in CHO cells B 8 pKi 10 nM Ki J. Med. Chem. (2008) 51: 6359-6370 [PMID:18817363]
ChEMBL Displacement of [3H]prazosin from human adrenergic Alpha-1B expressed in CHO cells B 8 pKi 10 nM Ki Bioorg. Med. Chem. (2010) 18: 7065-7077 [PMID:20801662]
ChEMBL Displacement of [3H]prazosin from human recombinant alpha1B adrenergic receptor expressed in CHO cell membranes after 30 mins B 8 pKi 10 nM Ki J. Med. Chem. (2013) 56: 584-588 [PMID:23252794]
ChEMBL Affinity constant towards human recombinant Alpha-1B adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay B 8 pKi 10 nM Ki J. Med. Chem. (2003) 46: 1504-1511 [PMID:12672251]
ChEMBL Affinity constant on CHO cells expressing Human recombinant Alpha-1B adrenergic receptor B 8 pKi 10 nM Ki J. Med. Chem. (2002) 45: 1633-1643 [PMID:11931617]
ChEMBL Binding affinity measured in CHO cells expressing human cloned Alpha-1B adrenergic receptor expressed as pKi B 8 pKi 10 nM Ki J. Med. Chem. (2003) 46: 4895-4903 [PMID:14584940]
ChEMBL Binding affinity against Alpha-1B adrenergic receptor from human clone B 8 pKi 9.9 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Binding affinity was tested on human Alpha-1B adrenergic receptor B 8.6 pKi 2.51 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
GtoPdb - - 9 pKi - - - Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248];
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]
ChEMBL Displacement of [3H]prazosin from human recombinant adrenergic alpha-1B receptor expressed in CHO cell membranes incubated for 60 mins B 10.42 pKi 0.04 nM Ki J Med Chem (2020) 63: 433-439 [PMID:31834797]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL Antagonistic affinity tested against isolated Rat Spleen Alpha-1B adrenergic receptor F 8.16 pKd 6.92 nM Kd J. Med. Chem. (2002) 45: 1633-1643 [PMID:11931617]
ChEMBL Antagonistic activity at ADRA1B in rat spleen F 8.2 pKd 6.31 nM Kd Bioorg. Med. Chem. Lett. (2006) 16: 150-153 [PMID:16216506]
ChEMBL Antagonistic activity against (-)-phenylephrine-induced contraction of rat spleen (Alpha-1B adrenergic receptor ) F 8.21 pKd 6.17 nM Kd J. Med. Chem. (2003) 46: 1504-1511 [PMID:12672251]
ChEMBL Activity at adrenergic alpha 1B receptor assessed as antagonsim of phenylephrine-induced contraction of Sprague-Dawley rat spleen F 8.21 pKd 6.17 nM Kd J. Med. Chem. (2006) 49: 7140-7149 [PMID:17125266]
ChEMBL Binding affinity towards Alpha-1B adrenergic receptor native receptor in rat liver using [3H]prazosin as radioligand B 7.59 pKi 25.64 nM Ki J. Med. Chem. (1996) 39: 2253-2258 [PMID:8667368]
ChEMBL Overall binding displacement in tissues containing only the Alpha-1B adrenergic receptor (rat spleen, rat liver) B 8.1 pKi 8 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL Binding affinity against Alpha-1D adrenergic receptor, from human clones. B 9.1 pKi 0.8 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Displacement of [3H]prazosin from human recombinant alpha1D adrenergic receptor expressed in CHO cell membranes after 30 mins B 9.29 pKi 0.51 nM Ki J. Med. Chem. (2013) 56: 584-588 [PMID:23252794]
ChEMBL Displacement of [3H]prazosin from human cloned Alpha-1D adrenergic receptor B 9.29 pKi 0.51 nM Ki J. Med. Chem. (1999) 42: 4214-4224 [PMID:10514291]
ChEMBL Affinity constant towards human recombinant Alpha-1D adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay B 9.29 pKi 0.51 nM Ki J. Med. Chem. (2003) 46: 1504-1511 [PMID:12672251]
ChEMBL Affinity constant on CHO cells expressing Human recombinant Alpha-1D adrenergic receptor B 9.29 pKi 0.51 nM Ki J. Med. Chem. (2002) 45: 1633-1643 [PMID:11931617]
ChEMBL Binding affinity measured in CHO cells expressing human cloned Alpha-1D adrenergic receptor expressed as pKi B 9.29 pKi 0.51 nM Ki J. Med. Chem. (2003) 46: 4895-4903 [PMID:14584940]
ChEMBL Displacement of [3H]prazosin from human cloned alpha1D adrenoceptor expressed in CHO cells B 9.29 pKi 0.51 nM Ki J. Med. Chem. (2008) 51: 6359-6370 [PMID:18817363]
ChEMBL Displacement of [3H]prazosin from human adrenergic Alpha-1D expressed in CHO cells B 9.29 pKi 0.51 nM Ki Bioorg. Med. Chem. (2010) 18: 7065-7077 [PMID:20801662]
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 9.29 pKi 9.29 nM Log Ki J. Med. Chem. (1999) 42: 2961-2968 [PMID:10425105]
ChEMBL Binding affinity was tested on human Alpha-1D adrenergic receptor B 9.6 pKi 0.25 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
GtoPdb - - 9.6 pKi - - - Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248];
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
ChEMBL Antagonistic activity against (-)-noradrenaline-induced contraction of rat thoracic aorta (Alpha-1D adrenergic receptor) F 8.6 pKd 2.51 nM Kd J. Med. Chem. (2003) 46: 1504-1511 [PMID:12672251]
ChEMBL Activity at adrenergic alpha 1D receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat thoracic aorta F 8.6 pKd 2.51 nM Kd J. Med. Chem. (2006) 49: 7140-7149 [PMID:17125266]
ChEMBL Antagonistic affinity tested against isolated Rat Thoracic Aorta Alpha-1D adrenergic receptor F 8.8 pKd 1.58 nM Kd J. Med. Chem. (2002) 45: 1633-1643 [PMID:11931617]
ChEMBL Antagonistic activity at ADRA1D in rat thoracic aorta F 8.8 pKd 1.58 nM Kd Bioorg. Med. Chem. Lett. (2006) 16: 150-153 [PMID:16216506]
ChEMBL Binding affinity towards Alpha-1D adrenergic receptor in rat brain using [3H]prazosin as radioligand B 8.2 pKi 6.26 nM Ki J. Med. Chem. (1996) 39: 2253-2258 [PMID:8667368]
ChEMBL Binding affinity against Alpha-1D adrenergic receptor, from rat clones. B 8.92 pKi 1.2 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Binding affinity against Alpha-2A adrenergic receptor, from human clones. B 8.46 pKi 3.5 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
GtoPdb - - 8.9 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470];
Mol Pharmacol (1992) 42: 1-5 [PMID:1353247];
Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642]
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909]
ChEMBL Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens F 6.59 pKd 257.04 nM Kd J. Med. Chem. (2006) 49: 7140-7149 [PMID:17125266]
ChEMBL The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones. B 7.34 pKi 46 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL Binding affinity against Alpha-2B adrenergic receptor from human clones. B 7.55 pKi 28 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
GtoPdb - - 8.4 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470];
Mol Pharmacol (1992) 42: 1-5 [PMID:1353247];
Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642]
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Binding affinity against Alpha-2C adrenergic receptor from human clones. B 9.1 pKi 0.8 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
GtoPdb - - 9.4 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470];
Mol Pharmacol (1992) 42: 1-5 [PMID:1353247];
Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642]
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 6.91 pKi 123.03 nM Ki J. Med. Chem. (1999) 42: 4214-4224 [PMID:10514291]
ChEMBL The binding affinity was evaluated on Dopamine receptor D2 expressed in rat striatum by using [3H]spiperone as radioligand B 6.91 pKi 6.91 nM Log Ki J. Med. Chem. (1999) 42: 2961-2968 [PMID:10425105]
ChEMBL Binding affinity towards Dopamine receptor D2 in rat striatum using [3H]spiperone as radioligand B 6.91 pKi 122.8 nM Ki J. Med. Chem. (1996) 39: 2253-2258 [PMID:8667368]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. B 6.97 pKi 107 nM Ki J. Med. Chem. (1993) 36: 1499-1500 [PMID:8098771]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL The binding affinity was evaluated on cloned human 5-hydroxytryptamine 1A receptor expressed in HeLa cells by using DPAT as radioligand. B 8.68 pKi 8.68 nM Log Ki J. Med. Chem. (1999) 42: 2961-2968 [PMID:10425105]
ChEMBL Displacement of [3H]8-hydroxy-2-(di-n-propylamino)tetralin from human 5-hydroxytryptamine 1A receptor B 8.68 pKi 2.09 nM Ki J. Med. Chem. (1999) 42: 4214-4224 [PMID:10514291]
ChEMBL Affinity constant on CHO cells expressing Human recombinant 5-hydroxytryptamine receptor 1A B 8.68 pKi 2.09 nM Ki J. Med. Chem. (2002) 45: 1633-1643 [PMID:11931617]
ChEMBL Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in human HeLa cells B 8.68 pKi 2.09 nM Ki J. Med. Chem. (2008) 51: 6359-6370 [PMID:18817363]
ChEMBL Displacement of [3H]8-OH-DPAT from human adrenergic 5HT1A expressed in human HeLa cells cells B 8.68 pKi 2.09 nM Ki Bioorg. Med. Chem. (2010) 18: 7065-7077 [PMID:20801662]
ChEMBL Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HeLa cell membranes after 30 mins B 8.68 pKi 2.09 nM Ki J. Med. Chem. (2013) 56: 584-588 [PMID:23252794]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor in rat hypocampus membrane using [3H]8-OH-DPAT as radioligand B 8.14 pKi 7.26 nM Ki J. Med. Chem. (1996) 39: 2253-2258 [PMID:8667368]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor by the displacement of [125I]trans-8-OH-PIPAT in membrane homogenates of hippocampal tissue of rat brain B 8.57 pKi 2.68 nM Ki J. Med. Chem. (1993) 36: 3161-3165 [PMID:8230102]
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 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]