WB 4101 [Ligand Id: 499] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL25554 (WB-4101) |
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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]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| ChEMBL | Antagonist activity at human recombinant alpha1A adrenoceptor assessed as inhibition of epinephrine-induced intracellular Ca2+ release | F | 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 | F | 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]; Br J Pharmacol (1997) 122: 849-58 [PMID:9384500] |
| 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]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| 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]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| 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 | - | - | - |
Mol Pharmacol (1992) 42: 1-5 [PMID:1353247]; Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642]; Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| 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]; Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| 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]; Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| 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 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]
