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ChEMBL ligand: CHEMBL13647 (BMY-7378) |
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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]