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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 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]