8-OH-DPAT [Ligand Id: 7] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL56 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Displacement of [3H]WAY100635 from human recombinant 5HT1A receptor | B | 5.4 | pKi | 3981.07 | nM | Ki | J Med Chem (2008) 51: 2887-2890 [PMID:18433113] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human cloned 5-HT1A receptor expressed in human HeLa cells | B | 5.48 | pKi | 3300 | nM | Ki | J Med Chem (2008) 51: 7602-7613 [PMID:19053888] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells after 120 mins | B | 8.29 | pKi | 5.1 | nM | Ki | J Med Chem (2008) 51: 1492-1495 [PMID:18269229] |
| ChEMBL | Binding affinity to 5-HT1A receptor (unknown origin) assessed as inhibition constant | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2022) 65: 10755-10808 [PMID:35939391] |
| 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 | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (2004) 47: 1900-1918 [PMID:15055991] |
| ChEMBL | Displacement of [3H]-OH-DPAT from human recombinant 5HT1A receptor expressed in HeLa cells after 30 mins by liquid scintillation counting | B | 8.43 | pKi | 3.71 | nM | Ki | J Med Chem (2012) 55: 23-36 [PMID:22145629] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor expressed in human HeLa cells | B | 8.43 | pKi | 3.71 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 2017-2020 [PMID:20185311] |
| ChEMBL | Displacement of [3H]8-hydroxy-2-(di-n-propylamino)tetralin from human 5-hydroxytryptamine 1A receptor | B | 8.46 | pKi | 3.47 | nM | Ki | J Med Chem (1999) 42: 4214-4224 [PMID:10514291] |
| ChEMBL | Binding affinity on human cloned 5-hydroxytryptamine 1A receptor transfected in human cell lines(He La) | B | 8.46 | pKi | 3.44 | nM | Ki | J Med Chem (2001) 44: 4431-4442 [PMID:11728188] |
| ChEMBL | Binding affinity towards human cloned 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand | B | 8.46 | pKi | 3.44 | nM | Ki | J Med Chem (2001) 44: 2403-2410 [PMID:11448222] |
| ChEMBL | The binding affinity was evaluated on cloned human 5-hydroxytryptamine 1A receptor expressed in HeLa cells by using DPAT as radioligand. | B | 8.47 | pKi | 8.47 | nM | Log Ki | J Med Chem (1999) 42: 2961-2968 [PMID:10425105] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HeLa cells after 30 mins | B | 8.47 | pKi | 3.39 | nM | Ki | ACS Med Chem Lett (2012) 3: 535-539 [PMID:24900506] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HeLa cell membranes after 30 mins | B | 8.47 | pKi | 3.39 | nM | Ki | J Med Chem (2013) 56: 584-588 [PMID:23252794] |
| 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 | 8.47 | pKi | 3.39 | nM | Ki | Eur J Med Chem (2019) 168: 461-473 [PMID:30844609] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in human HeLa cells | B | 8.47 | pKi | 3.39 | 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 | 8.47 | pKi | 3.39 | nM | Ki | Eur J Med Chem (2017) 125: 233-244 [PMID:27662034] |
| ChEMBL | Binding affinity at human 5HT1A receptor | B | 8.47 | pKi | 3.39 | nM | Ki | ACS Med Chem Lett (2013) 4: 875-879 [PMID:24900763] |
| ChEMBL | Displacement of 8-OH-DPAT from human 5-hydroxytryptamine 1A receptor expressed in chinese hamster ovary cells | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2005) 48: 3467-3470 [PMID:15887953] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in CHO cells | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2008) 51: 6980-7004 [PMID:18834188] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from recombinant human 5-HT1A receptor expressed in CHOK1 cell membranes after 1 hr by liquid scintillation counting method | B | 8.58 | pKi | 2.65 | nM | Ki | Bioorg Med Chem (2017) 25: 1250-1259 [PMID:28063784] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry | B | 8.58 | pKi | 2.65 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 4052-4056 [PMID:27396505] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in CHO-K1 cells incubated for 60 mins by liquid scintillation counting method | B | 8.58 | pKi | 2.65 | nM | Ki | Eur J Med Chem (2019) 183: 111690-111690 [PMID:31526973] |
| ChEMBL | Displacement of [3H]-5-HT from human 5-HT1A receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis | B | 8.58 | pKi | 2.65 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 1427-1430 [PMID:25759032] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HEK293 cells | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (2007) 50: 4214-4221 [PMID:17649988] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 cells | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (2008) 51: 5813-5822 [PMID:18800769] |
| ChEMBL | Binding affinity against human 5-hydroxytryptamine 1A receptor | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | In vivo binding affinity towards [3H]8-OH-DPAT-labeled 5-hydroxytryptamine 1A receptor sites in bovine hippocampus. | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (1993) 36: 671-682 [PMID:8459396] |
| ChEMBL | Compound was evaluated for the binding affinity against [3H]8-OH-DPAT-labeled 5-hydroxytryptamine 1A receptor in bovine hippocampus | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (1993) 36: 1053-1068 [PMID:8097537] |
| ChEMBL | Binding affinity against [3H]8-OH-DPAT-labeled 5-hydroxytryptamine 1A receptor sites in bovine hippocampus | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (1993) 36: 1069-1083 [PMID:8097538] |
| ChEMBL | Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand | B | 8.83 | pKi | 1.49 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1407-1412 [PMID:9871775] |
| ChEMBL | Binding affinity to 5HT1A receptor | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (2011) 54: 3086-3090 [PMID:21469694] |
| ChEMBL | Binding affinity to 5HT1A receptor | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2010) 53: 1319-1328 [PMID:20041669] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor expressed in CHO cells by liquid scintillation counting | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2010) 53: 1319-1328 [PMID:20041669] |
| ChEMBL | Binding affinity to 5-HT1A (unknown origin) | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127325-127325 [PMID:32631530] |
| ChEMBL | Receptor Binding Assay: 5-HT1A: Radioligand binding was performed using membranes from CHO-K1 cells stably transfected with the human 5-HT1A receptor. All assays were carried out in duplicates. 50 μL working solution of the tested compounds, 50 μL [3H]-8-OH-DPAT (final concentration 1 nM, Kd 0.8 nM) and 150 μL diluted membranes (10 μg protein per well) prepared in assay buffer (50 mM Tris-HCl, pH 7.4, 10 mM MgCl2, 0.1 mM EDTA, 0.1% ascorbic acid) were transferred to polypropylene 96-well microplate using 96-wells pipetting station Rainin Liquidator (MettlerToledo). Serotonin (10 μM) was used to define nonspecific binding. Microplate was covered with a sealing tape, mixed and incubated for 60 minutes at 27° C. The reaction was terminated by rapid filtration through GF/C filter mate presoaked with 0.3% polyethyleneimine for 30 minutes. Ten rapid washes with 200 μL 50 mM Tris-HCl buffer (4° C., pH 7.4) were performed using automated harvester system Harvester-96 MACH III FM (Tomtec). The filter mates were dried at 37° C. in forced air fan incubator and then solid scintillator MeltiLex was melted on filter mates at 90° C. for 5 minutes. Radioactivity was counted in MicroBeta2 scintillation counter (PerkinElmer) at approximately 30% efficiency. Data were fitted to a one-site curve-fitting equation with Prism 6 (GraphPad Software) and Ki values were estimated from the Cheng-Prusoff equation. | B | 9.05 | pKi | 0.9 | nM | Ki | US-10562853-B2. Compounds for treating disorders sensitive to serotoninergic regulation controlled by the 5-HT1A receptors (2020) |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from 5-HT1A receptor (unknown origin) assessed as inhibition binding | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2024) 67: 6144-6188 [PMID:38593423] |
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 1A receptor was determined using [3H]8-OH-DPAT-as radioligand | B | 9.08 | pKi | 0.83 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 793-795 [PMID:11277522] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from recombinant human 5HT1A receptor stably expressed in CHO-K1 cell membranes measured after 60 mins by microbeta2 scintillation counting method | B | 9.09 | pKi | 0.81 | nM | Ki | J Med Chem (2019) 62: 2750-2771 [PMID:30721053] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor stably expressed in CHO-K1 cell membranes measured after 60 mins by Microbeta2 scintillation counting method | B | 9.09 | pKi | 0.81 | nM | Ki | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| ChEMBL | Displacement of [3H]-WAY100635 from human 5-HT1A receptor expresssed in stable CHO cell membrane incubated for 90 mins by microbeta counting method | B | 9.1 | pKi | 0.8 | nM | Ki | Bioorg Med Chem (2020) 28: 115578-115578 [PMID:32631561] |
| ChEMBL | Binding affinity to human 5HT1A receptor | B | 9.1 | pKi | 0.8 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127053-127053 [PMID:32107165] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor | B | 9.1 | pKi | 0.79 | nM | Ki | J Med Chem (2008) 51: 2887-2890 [PMID:18433113] |
| ChEMBL | Displacement of [3H]8-OH-DAPT from human recombinant 5-HT1A receptor expressed in HEK cells measured after 60 to 90 mins by radioligand completion assay relative to control | B | 9.12 | pKi | 0.75 | nM | Ki | J Med Chem (2021) 64: 13510-13523 [PMID:34467758] |
| ChEMBL | Displacement of [3H]Way100635 from human recombinant 5-HT1A receptor expressed in CHO cell membranes by radioligand binding assay | B | 9.15 | pKi | 0.71 | nM | Ki | J Nat Prod (2015) 78: 722-729 [PMID:25695425] |
| ChEMBL | Displacement of radiolabeled 8OH-DPAT from human 5HT1A receptor | B | 9.18 | pKi | 0.66 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Binding affinity against [3H]- -8-OH-DPAT -labeled 5-hydroxytryptamine 1A sites in cloned CHO cells | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (1993) 36: 2208-2218 [PMID:8340922] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK-293 cells | B | 9.4 | pKi | 0.4 | nM | Ki | Eur J Med Chem (2015) 92: 221-235 [PMID:25557493] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human recombinant 5-HT1A receptor expressed in HEK293 cells | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2014) 57: 4543-4557 [PMID:24805037] |
| ChEMBL | Tested in vitro for the inhibition of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor, expressed in cloned CHO cells. | B | 9.4 | pKi | 0.4 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2759-2764 |
| GtoPdb | - | - | 9.4 | pKi | 0.4 | nM | Ki |
Biochem J (1992) 285 ( Pt 3): 933-8 [PMID:1386736]; Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 205-17 [PMID:9550290]; Biosci Rep (2004) 24: 101-15 [PMID:15628665]; J Pharmacol Exp Ther (1998) 284: 1082-94 [PMID:9495870]; Synapse (2000) 35: 79-95 [PMID:10611634]; Biochem Pharmacol (2003) 65: 435-40 [PMID:12527336]; J Pharmacol Exp Ther (1997) 280: 1241-9 [PMID:9067310] |
| ChEMBL | Binding affinity to 5HT1A receptor (unknown origin) assessed as inhibition constant | B | 9.51 | pKi | 0.31 | nM | Ki | ACS Chem Biol (2017) 12: 2619-2630 [PMID:28849908] |
| ChEMBL | Binding affinity to human 5-HT1A receptor by radioligand displacement assay | B | 9.68 | pKi | 0.21 | nM | Ki | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Displacement of [3H]OH-DPAT from human recombinant 5-HT1A receptor measured after 60 mins by scintillation counter method | B | 9.74 | pKi | 0.18 | nM | Ki | Eur J Med Chem (2019) 176: 292-309 [PMID:31112891] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor | B | 9.77 | pKi | 0.17 | nM | Ki | J Med Chem (2011) 54: 5320-5334 [PMID:21726069] |
| ChEMBL | Binding affinity to human 5-HT1A receptor extracted from HEK293 cell membrane assessed as inhibition of [3H]-OH-DPAT binding to 5-HT1A by measuring inhibition constant at 1 uM incubated for 1 hrs by microbeta2 reader | B | 9.8 | pKi | 0.16 | nM | Ki | Bioorg Med Chem (2024) 104: 117698-117698 [PMID:38552597] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem (2013) 21: 7604-7611 [PMID:24262884] |
| ChEMBL | Displacement of radiolabeled 8OH-DPAT from human 5HT1A receptor | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Inhibition of 5HT1A receptor (unknown origin) | B | 9.17 | pIC50 | 0.67 | nM | IC50 | ACS Chem Biol (2017) 12: 2619-2630 [PMID:28849908] |
| ChEMBL | Percent inhibition against 5-hydroxytryptamine 1A receptor at 1 uM | B | 9.18 | pIC50 | 0.66 | nM | IC50 | J Med Chem (2005) 48: 6887-6896 [PMID:16250647] |
| ChEMBL | Inhibition of human 5HT1A receptor | B | 9.23 | pIC50 | 0.59 | nM | IC50 | J Med Chem (2008) 51: 4150-4169 [PMID:18588282] |
| ChEMBL | Displacement of [3H]8-OHDPAT from human recombinant 5-HT1A receptor expressed in HEK293 cells | B | 9.28 | pIC50 | 0.53 | nM | IC50 | Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method | B | 9.28 | pIC50 | 0.53 | nM | IC50 | Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250] |
| ChEMBL | Binding affinity to human 5-HT1A receptor by radioligand displacement assay | B | 9.29 | pIC50 | 0.51 | nM | IC50 | Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449] |
| ChEMBL | Binding affinity to human 5-HT1A receptor by radioligand displacement assay | B | 9.48 | pIC50 | 0.33 | nM | IC50 | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Displacement of [3H]OH-DPAT from human recombinant 5-HT1A receptor measured after 60 mins by scintillation counter method | B | 9.55 | pIC50 | 0.28 | nM | IC50 | Eur J Med Chem (2019) 176: 292-309 [PMID:31112891] |
| ChEMBL | Agonist activity at human 5-HT1A receptor expressed in CHO cells after 90 mins by beta-arrestin-2 recruitment assay | B | 7.29 | pEC50 | 51.29 | nM | EC50 | Bioorg Med Chem (2015) 23: 4824-4830 [PMID:26081758] |
| ChEMBL | Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.49 | pEC50 | 32.36 | nM | EC50 | J Med Chem (2007) 50: 5024-5033 [PMID:17803293] |
| ChEMBL | Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay | F | 7.5 | pEC50 | 31.62 | nM | EC50 | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| ChEMBL | Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay | F | 7.5 | pEC50 | 31.62 | nM | EC50 | J Med Chem (2019) 62: 2750-2771 [PMID:30721053] |
| ChEMBL | Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding | F | 7.55 | pEC50 | 28.18 | nM | EC50 | J Med Chem (2007) 50: 865-876 [PMID:17300168] |
| ChEMBL | Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding | F | 7.59 | pEC50 | 26 | nM | EC50 | J Med Chem (2008) 51: 6980-7004 [PMID:18834188] |
| ChEMBL | Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay | F | 7.66 | pEC50 | 21.88 | nM | EC50 | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| ChEMBL | Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation | F | 7.82 | pEC50 | 15 | nM | EC50 | Eur J Med Chem (2013) 60: 42-50 [PMID:23279866] |
| ChEMBL | Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay | B | 7.84 | pEC50 | 14.45 | nM | EC50 | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| ChEMBL | Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay | B | 7.84 | pEC50 | 14.45 | nM | EC50 | J Med Chem (2019) 62: 2750-2771 [PMID:30721053] |
| ChEMBL | Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA | F | 7.92 | pEC50 | 12.02 | nM | EC50 | Bioorg Med Chem (2015) 23: 4824-4830 [PMID:26081758] |
| ChEMBL | In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells | F | 7.96 | pEC50 | 10.9 | nM | EC50 | J Med Chem (2005) 48: 3467-3470 [PMID:15887953] |
| ChEMBL | Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay | B | 8.09 | pEC50 | 8.13 | nM | EC50 | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| ChEMBL | Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay | B | 8.09 | pEC50 | 8.13 | nM | EC50 | J Med Chem (2019) 62: 2750-2771 [PMID:30721053] |
| ChEMBL | Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA | F | 8.1 | pEC50 | 8 | nM | EC50 | J Med Chem (2013) 56: 7851-7861 [PMID:24050112] |
| ChEMBL | Agonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assay | F | 8.22 | pEC50 | 6 | nM | EC50 | Bioorg Med Chem Lett (2019) 29: 126667-126667 [PMID:31547945] |
| ChEMBL | EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor | F | 8.24 | pEC50 | 5.82 | nM | EC50 | J Med Chem (2000) 43: 4701-4710 [PMID:11101361] |
| ChEMBL | Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay | F | 8.48 | pEC50 | 3.3 | nM | EC50 | Eur J Med Chem (2022) 229: 114045-114045 [PMID:34922191] |
| ChEMBL | In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor | F | 8.59 | pEC50 | 2.6 | nM | EC50 | J Med Chem (2005) 48: 3467-3470 [PMID:15887953] |
| 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Binding affinity against the site labelled by the 5-hydroxytryptamine 1A receptor agonist [3H]- 8-OH-DPAT | B | 8.6 | pKd | 2.5 | nM | Kd | J Med Chem (1994) 37: 4346-4351 [PMID:7996545] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor sites, in rat striatum membranes using [3H]- sandoz 205-501 as radioligand | B | 6.01 | pKi | 975 | nM | Ki | J Med Chem (1990) 33: 1541-1544 [PMID:2140413] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from rat cerebral cortex 5HT1A receptor measured after 15 mins by liquid scintillation counter method | B | 8.03 | pKi | 9.4 | nM | Ki | Bioorg Med Chem (2016) 24: 3994-4007 [PMID:27377863] |
| ChEMBL | In vitro binding affinity against 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT (agonist) as radioligand (sc) | B | 8.06 | pKi | 8.7 | nM | Ki | J Med Chem (1993) 36: 2059-2065 [PMID:8340910] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1A receptor in homogenated rat brain tissue, using by [3H]8-OH-DPAT as radioligand | B | 8.06 | pKi | 8.7 | nM | Ki | J Med Chem (1993) 36: 3409-3416 [PMID:8230131] |
| ChEMBL | Displacement of the radioligand [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor | B | 8.06 | pKi | 8.7 | nM | Ki | J Med Chem (1994) 37: 3263-3273 [PMID:7932553] |
| ChEMBL | Binding affinity was tested on 5-hydroxytryptamine 1A receptor using radioligand [3H]5-HT binding assay. | B | 8.37 | pKi | 4.3 | nM | Ki | J Med Chem (1996) 39: 4255-4260 [PMID:8863803] |
| ChEMBL | Displacement of [3H]5-HT from rat hippocampal 5-hydroxytryptamine 1A receptor with 10e-6 M ketanserin | B | 8.37 | pKi | 4.3 | nM | Ki | J Med Chem (1996) 39: 176-182 [PMID:8568804] |
| ChEMBL | Displacement of radioligand [3H]2-(di-N-propylamino)-8-hydroxytetralin from 5-hydroxytryptamine 1A receptor in rat frontal cortex homogenate | B | 8.55 | pKi | 2.8 | nM | Ki | J Med Chem (1993) 36: 2751-2760 [PMID:8410989] |
| ChEMBL | The compound was tested for binding affinity on [3H]8-OH-DPAT as specific ligand on 5-hydroxytryptamine 1A receptor in rat hippocampus | B | 8.63 | pKi | 2.33 | nM | Ki | J Med Chem (1999) 42: 173-177 [PMID:9888842] |
| ChEMBL | The compound was evaluated for binding affinity against 5-hydroxytryptamine 1A receptor in rat hippocampal membranes using [3H]8-OH-DPAT as radioligand in the presence of 3*10e-5 M GTP gamma S | B | 8.65 | pKi | 2.26 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 2035-2038 |
| ChEMBL | Binding affinity of compound against 5-hydroxytryptamine 1A receptor binding site using radioligand [3H]8-OH-DPAT | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (1989) 32: 1959-1962 [PMID:2569041] |
| ChEMBL | Binding was determined on 5-hydroxytryptamine 1A receptor in rat hippocampal membranes | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (2001) 44: 4431-4442 [PMID:11728188] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor from rat hippocampal membranes | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (2002) 45: 5727-5735 [PMID:12477356] |
| ChEMBL | Binding affinity against the 5-hydroxytryptamine 1A receptor labelled with [3H]8-OH-DPAT in rat hippocampal homogenates | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (1998) 41: 4995-5001 [PMID:9836617] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor of rat cortex membranes | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2003) 46: 3555-3558 [PMID:12877594] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1A receptor by displacing [3H]8-OH-DPAT radioligand in rat cortex membrane | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2002) 45: 3603-3611 [PMID:12166933] |
| ChEMBL | Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand. | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor in rat cerebral cortex | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 171-173 [PMID:12482417] |
| ChEMBL | Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement | B | 8.73 | pKi | 1.86 | nM | Ki | J Med Chem (1996) 39: 126-134 [PMID:8568799] |
| ChEMBL | Binding affinity for 5-hydroxytryptamine 1A receptor with [3H]5-HT | B | 8.8 | pKi | 1.59 | nM | Ki | J Med Chem (1994) 37: 105-112 [PMID:8289183] |
| ChEMBL | Inhibitory affinity constant against 5-hydroxytryptamine 1A receptor | B | 8.84 | pKi | 1.44 | nM | Ki | J Med Chem (1995) 38: 1701-1710 [PMID:7752194] |
| ChEMBL | In vitro ability to displace [3H]8-hydroxy-2-(di-n-propylamino) tetralin binding from 5-hydroxytryptamine 1A receptor site. | B | 8.84 | pKi | 1.44 | nM | Ki | J Med Chem (1992) 35: 2369-2374 [PMID:1535661] |
| ChEMBL | Binding affinity for rat cortex 5-hydroxytryptamine 1A receptor, by displacement of 0.2 nM [3H]8-OH-DPAT radioligand | B | 8.85 | pKi | 1.41 | nM | Ki | J Med Chem (1998) 41: 5070-5083 [PMID:9836623] |
| ChEMBL | Binding affinity to 5HT1A receptor in rat cortex membrane | B | 8.85 | pKi | 1.41 | nM | Ki | J Med Chem (2007) 50: 5024-5033 [PMID:17803293] |
| ChEMBL | Displacement of [3H]OH-DPAT from rat cortex 5HT1A receptor | B | 8.85 | pKi | 1.41 | nM | Ki | J Med Chem (2007) 50: 865-876 [PMID:17300168] |
| ChEMBL | In vitro by displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor on rat cortical membrane | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (1997) 40: 586-593 [PMID:9046349] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5-HT1A receptor in Wistar rat cerebral hippocampus membrane after 10 mins | B | 8.92 | pKi | 1.2 | nM | Ki | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Binding affinity to the rat 5-hydroxytryptamine 1A receptor | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2003) 46: 646-649 [PMID:12570387] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from 5-HT1A receptor in rat hippocampal membranes | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2017) 60: 2605-2628 [PMID:28244748] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor in Wistar Han rat hippocampal membranes | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2004) 47: 6616-6624 [PMID:15588097] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (1988) 31: 867-870 [PMID:2965244] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor of rat hippocampus mambranes | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
| ChEMBL | Binding affinity at [3H]8-OH-DPAT-Labeled 5-hydroxytryptamine 1A receptor sites in rat brain hippocampal membranes | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (1989) 32: 253-256 [PMID:2521252] |
| ChEMBL | In vitro ability to displace [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor sites of rat brain cortex. | B | 8.93 | pKi | 1.18 | nM | Ki | J Med Chem (1995) 38: 1273-1277 [PMID:7731013] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from rat hippocampal 5-hydroxytryptamine 1A receptor | B | 8.96 | pKi | 1.09 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 2035-2038 |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from 5-HT1A receptor in Sprague-Dawley rat cerebral cortex after 15 mins | B | 8.99 | pKi | 1.02 | nM | Ki | J Med Chem (2013) 56: 7851-7861 [PMID:24050112] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor sites in cortical membranes using [3H]8-OH-DPAT as radioligand | B | 9 | pKi | 1 | nM | Ki | J Med Chem (1990) 33: 1541-1544 [PMID:2140413] |
| ChEMBL | Affinity for 5-hydroxytryptamine 1A receptor site | B | 9 | pKi | 1 | nM | Ki | J Med Chem (1989) 32: 2311-2318 [PMID:2795604] |
| ChEMBL | Displacement of [3H]8OH-DPAT from 5HT1A in Sprague-Dawley rat brain cortex by liquid scintillation counting | B | 9.1 | pKi | 0.8 | nM | Ki | Eur J Med Chem (2010) 45: 752-759 [PMID:19954866] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from Sprague-Dawley rat brain cortex serotonin 5-HT1A receptor after 30 mins by liquid scintillation counting | B | 9.1 | pKi | 0.8 | nM | Ki | Eur J Med Chem (2012) 47: 520-529 [PMID:22133459] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat cortex membrane | B | 9.19 | pKi | 0.64 | nM | Ki | Bioorg Med Chem (2007) 15: 7581-7589 [PMID:17900912] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor by the displacement of [3H]8-OH-DPAT in membrane homogenates of hippocampal tissue of rat brain | B | 9.2 | pKi | 0.63 | nM | Ki | J Med Chem (1993) 36: 3161-3165 [PMID:8230102] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from rat hippocampal 5-hydroxytryptamine 1A receptor | B | 9.27 | pKi | 0.54 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 2035-2038 |
| ChEMBL | In vitro displacement of radioactively labeled ligand [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor site in CHO cells | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (1995) 38: 725-734 [PMID:7861420] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor of rat hippocampal membranes | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Binding affinity against rat 5-hydroxytryptamine 1A receptor | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1A receptor from CHO-K1 cells, using [3H]8-OH-DPAT as the radioligand. | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (1995) 38: 2202-2216 [PMID:7783152] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from rat striata 5-hydroxytryptamine 1A receptor | B | 9.33 | pKi | 0.47 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 509-512 [PMID:10743959] |
| ChEMBL | The compound was evaluated for binding affinity against 5-hydroxytryptamine 1A receptor in rat hippocampal membranes using [3H]8-OH-DPAT as radioligand in the presence of 1 mM of MnCl2 | B | 9.57 | pKi | 0.27 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 2035-2038 |
| ChEMBL | Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus | F | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor using receptor binding assay | B | 8.09 | pIC50 | 8.06 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 2857-2862 |
| ChEMBL | In vitro binding activity against 5-hydroxytryptamine 1A receptor from homogenized rat brain, using [3H]8-OH-DPAT as the radioligand | B | 8.35 | pIC50 | 4.46 | nM | IC50 | J Med Chem (1989) 32: 2273-2276 [PMID:2571729] |
| ChEMBL | The compound was tested in vitro for inhibitory activity against 5-HT1A receptor in rats, using [3H]8-OH-DPAT as radioligand | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (1992) 35: 3984-3990 [PMID:1433207] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand. | B | 8.52 | pIC50 | 3.02 | nM | IC50 | J Med Chem (1988) 31: 1087-1093 [PMID:3373482] |
| ChEMBL |
Concentration necessary to achieve half maximal inhibition of [3H]8-Hydroxy-2-(di-n-propylamino)tetralin binding to 5-hydroxytryptamine 1A receptor at 1 uM |
B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1989) 32: 720-727 [PMID:2537429] |
| ChEMBL | Binding affinity to 5-hydroxytryptamine 1A receptor in rat hippocampus membranes,3H-8-OH-DPAT and buspirone for nonspecific binding (NSB) | B | 8.62 | pIC50 | 2.4 | nM | IC50 | J Med Chem (1996) 39: 4285-4298 [PMID:8863806] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1A (5-HT1A) receptor in rat hippocampus membranes | B | 8.62 | pIC50 | 2.4 | nM | IC50 | J Med Chem (1994) 37: 1779-1793 [PMID:7912735] |
| ChEMBL | Binding affinity towards rat 5-hydroxytryptamine 1A receptor was evaluated using [3H]8-OH-DPAT as radioligand | B | 8.68 | pIC50 | 2.1 | nM | IC50 | J Med Chem (1996) 39: 4928-4934 [PMID:8960552] |
| ChEMBL | Binding affinity against serotonin 5-hydroxytryptamine 1A receptor in rat hippocampus membrane using [3H]8-OH-DPAT as radioligand | B | 8.68 | pIC50 | 2.1 | nM | IC50 | J Med Chem (1996) 39: 3195-3202 [PMID:8759642] |
| ChEMBL | In vitro ability to inhibit binding of radioligand [3H]8-OH-DPAT to 5-hydroxytryptamine 1A receptor in rat cerebral cortex | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (1994) 37: 99-104 [PMID:8289207] |
| ChEMBL | In vitro binding affinity measured on serotonin 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand. | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (1995) 38: 942-949 [PMID:7699710] |
| ChEMBL | Agonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysis | F | 7.85 | pEC50 | 14 | nM | EC50 | Bioorg Med Chem (2023) 96: 117518-117518 [PMID:37951135] |
| 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand. | B | 6.2 | pKi | 638 | nM | Ki | J Med Chem (1995) 38: 2202-2216 [PMID:7783152] |
| ChEMBL | Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand | B | 6.25 | pKi | 559 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1407-1412 [PMID:9871775] |
| GtoPdb | - | - | 6.2 | pIC50 | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (1997) 356: 328-34 [PMID:9303569] |
| ChEMBL | The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line | F | 6.59 | pEC50 | 260 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 1407-1412 [PMID:9871775] |
| 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
| ChEMBL | Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand. | B | 4.2 | pKi | 63000 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| ChEMBL | Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1988) 31: 867-870 [PMID:2965244] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 2035-2038 |
| ChEMBL | Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor | B | 5.59 | pKi | 2570 | nM | Ki | J Med Chem (1994) 37: 105-112 [PMID:8289183] |
| ChEMBL | Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand | B | 5.42 | pIC50 | 3801.89 | nM | IC50 | J Med Chem (1988) 31: 1087-1093 [PMID:3373482] |
| 5-HT1D receptor/5-hydroxytryptamine receptor 1D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1D receptor alpha expressed in CHO-K1 cells, using [3H]-5-HT as the radioligand. | B | 6.79 | pKi | 164 | nM | Ki | J Med Chem (1995) 38: 2202-2216 [PMID:7783152] |
| ChEMBL | Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1D receptor using [3H]-5-CT as radioligand | B | 6.94 | pKi | 115 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1407-1412 [PMID:9871775] |
| GtoPdb | - | - | 7.3 | pKi | - | - | - |
Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663]; Naunyn Schmiedebergs Arch Pharmacol (1997) 356: 328-34 [PMID:9303569]; Mol Pharmacol (1996) 50: 1567-80 [PMID:8967979] |
| 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| GtoPdb | - | - | 5.6 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| 5-hydroxytryptamine receptor 2A in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 2 receptor | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortex | B | 4.31 | pIC50 | 49000 | nM | IC50 | J Med Chem (1994) 37: 1779-1793 [PMID:7912735] |
| 5-HT2A receptor/5-hydroxytryptamine receptor 2A 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 | Binding affinity towards rat 5-hydroxytryptamine 2A receptor was evaluated using [3H]- ketanserin as radioligand | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1996) 39: 4928-4934 [PMID:8960552] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 2A receptor by displacement of [3H]-ketanserin from rat prefrontal cerebral cortex mambranes | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
| 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Inhibition of [3H]mesulergine binding to 5-hydroxytryptamine 1C receptor of pig choroid Plexus | B | 4.83 | pKi | 14800 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Evaluated for the binding affinity to porcine choroid plexus at 5-hydroxytryptamine 2C receptor binding site by using [3H]-MES as a radioligand. | B | 5.14 | pKi | 7250 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| GtoPdb | - | - | 5.6 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| 5-HT5A receptor/5-hydroxytryptamine receptor 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 5A receptor | B | 5.6 | pKi | 2500 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand | B | 5.6 | pKi | 2500 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| GtoPdb | - | - | 5.7 | pKi | - | - | - |
FEBS Lett (1994) 355: 242-6 [PMID:7988681]; Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685] |
| ChEMBL | Binding affinity for rodent 5-hydroxytryptamine 5A receptor | B | 6 | pKi | 1000 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| 5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966] | ||||||||
| GtoPdb | - | - | 5.9 | pKi | - | - | - |
Mol Pharmacol (1993) 43: 313-9 [PMID:8450829]; Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685] |
| 5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells | B | 6.3 | pKi | 501.19 | nM | Ki | Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003] |
| ChEMBL | Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor | B | 6.33 | pKi | 466 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis | B | 6.41 | pKi | 388 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 1427-1430 [PMID:25759032] |
| ChEMBL | Displacement of [3H]-5-HT from recombinant human 5-HT7A receptor expressed in CHOK1 cell membranes after 40 mins by liquid scintillation counting method | B | 6.41 | pKi | 388 | nM | Ki | Bioorg Med Chem (2017) 25: 1250-1259 [PMID:28063784] |
| ChEMBL | Displacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry | B | 6.41 | pKi | 388 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 4052-4056 [PMID:27396505] |
| GtoPdb | - | - | 7.6 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2001) 363: 620-32 [PMID:11414657]; Br J Pharmacol (1997) 122: 126-32 [PMID:9298538]; J Biol Chem (1993) 268: 23422-6 [PMID:8226867]; Br J Pharmacol (1998) 124: 1300-6 [PMID:9720804] |
| 5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304] | ||||||||
| GtoPdb | - | - | 6.6 | pKi | - | - | - | Mol Pharmacol (1993) 44: 229-36 [PMID:8394987] |
| 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
| ChEMBL | Binding affinity towards rat 5-hydroxytryptamine 7 receptor | B | 6.82 | pKi | 150 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| GtoPdb | - | - | 7.5 | pKi | - | - | - |
J Biol Chem (1993) 268: 18200-4 [PMID:8394362]; Proc Natl Acad Sci USA (1993) 90: 8547-51 [PMID:8397408] |
| α1A-adrenoceptor/Alpha-1A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| ChEMBL | Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand | B | 5.76 | pKi | 1757.2 | nM | Ki | J Med Chem (2001) 44: 2403-2410 [PMID:11448222] |
| ChEMBL | Binding affinity was determined on human cloned Alpha-1A adrenoceptor | B | 5.76 | pKi | 1757 | nM | Ki | J Med Chem (2001) 44: 4431-4442 [PMID:11728188] |
| 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 | 6 | pKi | <6 | nM | Log Ki | J Med Chem (1999) 42: 2961-2968 [PMID:10425105] |
| ChEMBL | Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor | B | 6 | pKi | <1000 | 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 | pKi | >1000 | nM | Ki | J Med Chem (2008) 51: 6359-6370 [PMID:18817363] |
| 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 | pKi | >1000 | nM | Ki | Eur J Med Chem (2019) 168: 461-473 [PMID:30844609] |
| ChEMBL | Radioligand Binding Assay: Alpha1-adrenergic Receptor: Radioligand binding was performed using tissue (rat cortex). All assays were carried out in duplicates. 50 μL working solution of the tested compounds, 50 μL [3H]-prazosin (final concentration 0.2 nM, Kd 0.2 nM) and 150 μL tissue suspension prepared in assay buffer (50 mM Tris-HCl, pH 7.6) were transferred to polypropylene 96well microplate using 96wells pipetting station Rainin Liquidator (MettlerToledo). Phentolamine (10 μM) was used to define nonspecific binding. Microplate was covered with a sealing tape, mixed and incubated for 30 minutes at 30° C. The reaction was terminated by rapid filtration through GF/B filter mate. Ten rapid washes with 200 μL 50 mM Tris-HCl buffer (4° C., pH 7.6) were performed using automated harvester system Harvester-96 MACH III FM (Tomtec). The filter mates were dried at 37° C. in forced air fan incubator and soaked in 10 mL of liquid scintillation cocktail Ultima Gold MV (PerkinElmer, USA). After even distribution of scintillation cocktail filter bag was sealed. Radioactivity was counted in MicroBeta2 scintillation counter (PerkinElmer) at approximately 30% efficiency. Data were fitted to a one-site curve-fitting equation with Prism 6 (Graph Pad Software) and Ki values were estimated from the Cheng-Prusoff equation. | B | 6 | pKi | >1000 | nM | Ki | US-10562853-B2. Compounds for treating disorders sensitive to serotoninergic regulation controlled by the 5-HT1A receptors (2020) |
| ChEMBL | Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2013) 56: 584-588 [PMID:23252794] |
| ChEMBL | Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells | B | 6.82 | pKi | 151.36 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 2017-2020 [PMID:20185311] |
| ChEMBL | Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting | B | 6.82 | pKi | 151.36 | nM | Ki | J Med Chem (2012) 55: 23-36 [PMID:22145629] |
| Alpha-1A adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130] | ||||||||
| ChEMBL | Binding affinity against alpha-1 adrenergic receptor in calf frontal cortex | B | 4.52 | pIC50 | 30000 | nM | IC50 | J Med Chem (1994) 37: 1779-1793 [PMID:7912735] |
| α1A-adrenoceptor/Alpha-1A adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens. | B | 5.68 | pKi | 2082 | nM | Ki | J Med Chem (2004) 47: 1900-1918 [PMID:15055991] |
| α1B-adrenoceptor/Alpha-1B adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| ChEMBL | Binding affinity towards human cloned alpha-1B-adrenoceptor using [3H]prazosin as radioligand | B | 5.22 | pKi | 5975 | nM | Ki | J Med Chem (2001) 44: 2403-2410 [PMID:11448222] |
| ChEMBL | Binding affinity was determined on human cloned alpha-1B adrenergic receptor | B | 5.22 | pKi | 5975 | nM | Ki | J Med Chem (2001) 44: 4431-4442 [PMID:11728188] |
| ChEMBL | Binding affinity constant against alpha-1B adrenergic receptor of guinea pig spleen | B | 5.73 | pKi | 1882 | nM | Ki | J Med Chem (2004) 47: 1900-1918 [PMID:15055991] |
| 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 | 6 | pKi | <6 | nM | Log Ki | J Med Chem (1999) 42: 2961-2968 [PMID:10425105] |
| ChEMBL | Displacement of [3H]prazosin from human recombinant alpha1B adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2012) 55: 23-36 [PMID:22145629] |
| ChEMBL | Displacement of [3H]prazosin from human recombinant alpha1B adrenergic receptor expressed in CHO cell membranes after 30 mins | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2013) 56: 584-588 [PMID:23252794] |
| ChEMBL | Displacement of [3H]prazosin from human cloned Alpha-1B adrenergic receptor | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1999) 42: 4214-4224 [PMID:10514291] |
| 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 | pKi | >1000 | nM | Ki | Eur J Med Chem (2019) 168: 461-473 [PMID:30844609] |
| ChEMBL | Displacement of [3H]prazosin from human cloned Alpha-1B adrenoceptor expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2008) 51: 6359-6370 [PMID:18817363] |
| ChEMBL | Displacement of [3H]prazosin from human Alpha-1B adrenergic receptor expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 2017-2020 [PMID:20185311] |
| α1D-adrenoceptor/Alpha-1D adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| 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 | 6 | pKi | <6 | nM | Log Ki | J Med Chem (1999) 42: 2961-2968 [PMID:10425105] |
| ChEMBL | Displacement of [3H]prazosin from human cloned Alpha-1D adrenergic receptor | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1999) 42: 4214-4224 [PMID:10514291] |
| ChEMBL | Binding affinity towarda alpha-1D adrenergic receptor | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2001) 44: 4431-4442 [PMID:11728188] |
| ChEMBL | Binding affinity towards human cloned alpha-1D-adrenoceptor using [3H]prazosin as radioligand | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2001) 44: 2403-2410 [PMID:11448222] |
| ChEMBL | Displacement of [3H]prazosin from human cloned alpha1D adrenoceptor expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2008) 51: 6359-6370 [PMID:18817363] |
| ChEMBL | Displacement of [3H]prazosin from human Alpha-1D adrenergic receptor expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 2017-2020 [PMID:20185311] |
| ChEMBL | Displacement of [3H]prazosin from human recombinant Alpha-1D adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting | B | 6 | pKi | >1000 | 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 | 6 | pKi | >1000 | nM | Ki | J Med Chem (2013) 56: 584-588 [PMID:23252794] |
| 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 | 6 | pKi | >1000 | nM | Ki | Eur J Med Chem (2019) 168: 461-473 [PMID:30844609] |
| α1D-adrenoceptor/Alpha-1D adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944] | ||||||||
| ChEMBL | Binding affinity to the adrenergic receptor alpha-1D of rat aorta | B | 5.27 | pKi | 5421 | nM | Ki | J Med Chem (2004) 47: 1900-1918 [PMID:15055991] |
| Alpha-2A adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4744] [UniProtKB: Q28838] | ||||||||
| ChEMBL | Binding affinity against alpha-2 adrenergic receptor in calf frontal cortex | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (1994) 37: 1779-1793 [PMID:7912735] |
| D(1A) dopamine receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136] | ||||||||
| ChEMBL | Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum | B | 4.06 | pKi | 87300 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| D1 receptor/D(1A) dopamine receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3071] [GtoPdb: 214] [UniProtKB: Q61616] | ||||||||
| ChEMBL | Binding affinity against Dopamine receptor D1 | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| D1 receptor/D(1A) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | In vitro binding activity against dopamine D1 receptor from homogenized rat brain, using [3H]SCH-23390 as the radioligand | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1989) 32: 2273-2276 [PMID:2571729] |
| D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Inhibitory activity against [125I]- NCQ298 binding to dopamine receptor D2 in Sf 9 cells | B | 5.49 | pKi | 3243 | nM | Ki | J Med Chem (1993) 36: 3161-3165 [PMID:8230102] |
| ChEMBL | Radioligand Binding Assay: D2 Dopamine Receptor:Radioligand binding was performed using membranes from CHO-K1 cells stably transfected with the human D2 receptor. All assays were carried out in duplicates. 50 μL working solution of the tested compounds, 50 μL [3H]-methylspiperon (final concentration 0.4 nM, Kd 0.4 nM) and 150 μL diluted membranes (10 μg protein per well) prepared in assay buffer (50 mM HEPES, pH 7.4, 50 mM NaCl, 5 mM MgCl2, 0.5 mM EDTA) were transferred to polypropylene 96well microplate using 96wells pipetting station Rainin Liquidator (MettlerToledo). (+)-butaclamol (10 μM) was used to define nonspecific binding. Microplate was covered with a sealing tape, mixed and incubated for 60 minutes at 37° C. The reaction was terminated by rapid filtration through GF/C filter mate presoaked with 0.3% polyethyleneimine for 30 minutes. Ten rapid washes with 200 μL 50 mM Tris buffer (4° C., pH 7.4) were performed using automated harvester system Harvester-96 MACH III FM (Tomtec). The filter mates were dried at 37° C. in forced air fan incubator and then solid scintillator MeltiLex was melted on filter mates at 90° C. for 5 minutes. Radioactivity was counted in MicroBeta2 scintillation counter (PerkinElmer) at approximately 30% efficiency. Data were fitted to a one-site curve-fitting equation with Prism 6 (GraphPad Software) and Ki values were estimated from the Cheng-Prusoff equation. | B | 6 | pKi | >1000 | nM | Ki | US-10562853-B2. Compounds for treating disorders sensitive to serotoninergic regulation controlled by the 5-HT1A receptors (2020) |
| ChEMBL | Binding affinity against [3H]U-86,170-labeled dopamine receptor D2 in cloned CHO cells | B | 7.07 | pKi | 86 | nM | Ki | J Med Chem (1993) 36: 1053-1068 [PMID:8097537] |
| ChEMBL | Binding affinity against [3H]U-86,170-labeled dopamine receptor D2 in cloned CHO cells | B | 7.07 | pKi | 86 | nM | Ki | J Med Chem (1993) 36: 1069-1083 [PMID:8097538] |
| ChEMBL | Binding affinity against Dopamine receptor D2 | B | 7.08 | pKi | 84 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Inhibitory concentration against binding of Dopamine receptor D2 by displacement of [3H]spiperone | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 509-512 [PMID:10743959] |
| D(2) dopamine receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288] | ||||||||
| ChEMBL | Inhibition of [3H]raclopride binding to Dopamine receptor D2 of bovine striatum | B | 5.62 | pKi | 2380 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Compound was evaluated for the binding affinity towards Dopamine receptor D2 using [3H]raclopride radioligand. | B | 6.1 | pIC50 | 800 | nM | IC50 | J Med Chem (1996) 39: 4285-4298 [PMID:8863806] |
| ChEMBL | Binding affinity against D2 receptor in calf caudate nucleus | B | 6.1 | pIC50 | 800 | nM | IC50 | J Med Chem (1994) 37: 1779-1793 [PMID:7912735] |
| D2 receptor/D(2) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | Binding affinity of compound against Dopamine receptor D2 binding site using radioligand [3H]spiperone | B | 5.46 | pKi | 3500 | nM | Ki | J Med Chem (1989) 32: 1959-1962 [PMID:2569041] |
| ChEMBL | Binding affinity against D2 receptor in homogenated rat brain tissue, using by [3H]spiperone as radioligand | B | 5.87 | pKi | 1357 | nM | Ki | J Med Chem (1993) 36: 3409-3416 [PMID:8230131] |
| ChEMBL | Displacement of [3H]spiperone from dopamine receptor D2 | B | 5.87 | pKi | 1357 | nM | Ki | J Med Chem (1993) 36: 2059-2065 [PMID:8340910] |
| ChEMBL | Displacement of the radioligand [3H]spiperone from D2 receptor | B | 5.87 | pKi | 1357 | nM | Ki | J Med Chem (1994) 37: 3263-3273 [PMID:7932553] |
| ChEMBL | Binding affinity against Dopamine receptor D2 from CHO-K1 cells, using [3H]U-86,170 as the radioligand. | B | 5.95 | pKi | 1126 | nM | Ki | J Med Chem (1995) 38: 2202-2216 [PMID:7783152] |
| ChEMBL | The binding affinity was evaluated on Dopamine receptor D2 expressed in rat striatum by using [3H]spiperone as radioligand | B | 6 | pKi | <6 | nM | Log Ki | J Med Chem (1999) 42: 2961-2968 [PMID:10425105] |
| ChEMBL | Binding affinity against [3H]raclopride-labeled dopamine receptor D2 in rat striatum. | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1993) 36: 1053-1068 [PMID:8097537] |
| ChEMBL | Displacement of [3H]spiperone from rat brain Dopamine receptor D2 | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1999) 42: 4214-4224 [PMID:10514291] |
| ChEMBL | Binding affinity for [3H]raclopride-labeled dopamine receptor D2 in rat striatum | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1993) 36: 1069-1083 [PMID:8097538] |
| ChEMBL | Displacement of [3H]YM-09151-2 from rat striatum D2 receptor | B | 6.26 | pKi | 549.54 | nM | Ki | J Med Chem (2007) 50: 865-876 [PMID:17300168] |
| ChEMBL | Displacement of [3H]U-86170 from Dopamine receptor D2 | B | 7.07 | pKi | 86 | nM | Ki | J Med Chem (1995) 38: 725-734 [PMID:7861420] |
| ChEMBL | Tested in vitro for the inhibition of [3H]raclopride binding to Dopamine receptor D2 in rat striatum | B | 7.07 | pKi | 86 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2759-2764 |
| ChEMBL | The compound was tested in vitro for inhibitory activity against dopamine receptor in rats using [3H]spiperone as radioligand | B | 5.24 | pIC50 | 5800 | nM | IC50 | J Med Chem (1992) 35: 3984-3990 [PMID:1433207] |
| ChEMBL | In vitro binding activity against Dopamine receptor D2 from homogenized rat brain, using [3H]spiperone as the radioligand | B | 5.24 | pIC50 | 5760 | nM | IC50 | J Med Chem (1989) 32: 2273-2276 [PMID:2571729] |
| ChEMBL | Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand | B | 8.28 | pIC50 | 5.2 | nM | IC50 | J Med Chem (1996) 39: 3195-3202 [PMID:8759642] |
| ChEMBL | Binding affinity towards rat Dopamine receptor D2 was evaluated using [3H]- spiroperidol as radioligand | B | 8.28 | pIC50 | 5.2 | nM | IC50 | J Med Chem (1996) 39: 4928-4934 [PMID:8960552] |
| D3 receptor/D(3) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Inhibition of [3H]spiperone binding to Dopamine receptor D3 in bovine cortex | B | 4.84 | pKi | 14600 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Tested in vitro for the inhibition of [3H]U-86170 binding to Dopamine receptor D3, expressed in cloned CHO cells | B | 6.59 | pKi | 259 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2759-2764 |
| D3 receptor/D(3) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
| ChEMBL | Binding affinity against Dopamine receptor D3 from CHO-K1 cells, using [3H]spiperone as the radioligand. | B | 6.48 | pKi | 333 | nM | Ki | J Med Chem (1995) 38: 2202-2216 [PMID:7783152] |
| ChEMBL | Inhibitory activity against [125I]- NCQ298 binding to dopamine receptor D3 in Sf 9 cells | B | 6.6 | pKi | 251 | nM | Ki | J Med Chem (1993) 36: 3161-3165 [PMID:8230102] |
| ChEMBL | Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. | B | 6.61 | pKi | 248 | nM | Ki | J Med Chem (1993) 36: 1499-1500 [PMID:8098771] |
| D4 receptor/D(4) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells | B | 5.82 | pKi | >1515 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2759-2764 |
| Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] | ||||||||
| ChEMBL | Binding affinity against norepinephrine transporter (NET) by displacement of [3H]nisoxetine in male wistar rats | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
| 5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16] | ||||||||
| ChEMBL | Ability to displace [3H]granisetron specifically bound to 5-hydroxytryptamine 3 receptor in rat cortical membrane | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (1998) 41: 728-741 [PMID:9513601] |
| sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | Binding affinity against sigma receptor | B | 5.61 | pKi | >2427 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] | ||||||||
| ChEMBL | Inhibition of [3H]DTG binding to sigma receptor in rat hippocampus | B | 5.28 | pKi | 5240 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| DAT/Sodium-dependent dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
| ChEMBL | Binding affinity against dopamine transporter (DAT) by displacement of [3H]WIN-35428 in male wistar rats | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
| SERT/Sodium-dependent serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Binding affinity against serotonin transporter (SERT) by displacement of [3H]paroxetine in male wistar rats | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
| 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| GtoPdb | - | - | 5.5 | pKi | - | - | - |
Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]; Eur J Pharmacol (2004) 484: 127-39 [PMID:14744596] |
| 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939] | ||||||||
| GtoPdb | - | - | 5.8 | pKi | - | - | - | Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639] |
| 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| GtoPdb | - | - | 5.4 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994] | ||||||||
| GtoPdb | - | - | 5.4 | pKi | - | - | - | Mol Pharmacol (1993) 43: 419-26 [PMID:8450835] |
ChEMBL data shown on this page come from version 36:
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]
