buspirone [Ligand Id: 36] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL49 (BCI-024, Buspirona, Buspirone, Gen-buspirone) |
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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 | Binding affinity to 5HT1A receptor | B | 8 | pKd | 10 | nM | Kd | J Med Chem (2009) 52: 6107-6125 [PMID:19754201] |
| ChEMBL | Displacement of [3H]-5-carboxamidotryptamine from human 5-HT1A receptor expressed in HEK293T cell membranes incubated for 90 mins by scintillation counting method | B | 7.3 | pKi | 50 | nM | Ki | Bioorg Med Chem (2020) 28: 115262-115262 [PMID:31882369] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from 5HT1A receptor (unknown origin) | B | 7.46 | pKi | 34.3 | nM | Ki | ACS Med Chem Lett (2017) 8: 390-394 [PMID:28435524] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells after 1 hr by microbeta plate reader analysis | B | 7.46 | pKi | 34.3 | nM | Ki | Eur J Med Chem (2020) 185: 111857-111857 [PMID:31734022] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counter method | B | 7.49 | pKi | 32.36 | nM | Ki | Eur J Med Chem (2019) 179: 1-15 [PMID:31229883] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counter method | B | 7.49 | pKi | 32.2 | nM | Ki | Eur J Med Chem (2019) 179: 1-15 [PMID:31229883] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human recombinant 5-HT1A receptor expressed in HEK293 cells after 1 hr by microbeta scintillation counting method | B | 7.49 | pKi | 32.2 | nM | Ki | Eur J Med Chem (2019) 170: 261-275 [PMID:30904783] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cell membranes assessed as inhibition constant incubated for 1 hr by Microbeta plate reader based analysis | B | 7.49 | pKi | 32 | nM | Ki | Eur J Med Chem (2023) 260: 115756-115756 [PMID:37657272] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from 5-HT1A receptor (unknown origin) assessed as inhibition constant by radioligand binding assay | B | 7.49 | pKi | 32 | nM | Ki | J Med Chem (2024) 67: 1580-1610 [PMID:38190615] |
| ChEMBL | Binding affinity to 5HT1A receptor | B | 7.62 | pKi | 24 | nM | Ki | J Med Chem (2010) 53: 1319-1328 [PMID:20041669] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human recombinant 5-HT1A receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis | B | 7.66 | pKi | 22 | nM | Ki | Eur J Med Chem (2014) 78: 324-339 [PMID:24691057] |
| ChEMBL | Displacement of [3H]5-carboxamidotryptamine to human 5HT1A expressed in HEK293 cells by filter binding assay | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2011) 54: 3206-3221 [PMID:21486038] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in CHO-K1 cell membranes incubated for 60 mins by microbeta scintillation counting analysis | B | 7.68 | pKi | 21 | nM | Ki | Eur J Med Chem (2019) 183: 111736-111736 [PMID:31586817] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method | B | 7.7 | pKi | 20 | nM | Ki | Eur J Med Chem (2020) 201: 112437-112437 [PMID:32673902] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor in HEK293 cells | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2006) 49: 3116-3135 [PMID:16722631] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor expressed in CHO cells by liquid scintillation counting | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2010) 53: 1319-1328 [PMID:20041669] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells | B | 7.7 | pKi | 20 | nM | Ki | Eur J Med Chem (2016) 112: 258-269 [PMID:26900658] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5HT1AR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting method | B | 7.7 | pKi | 20 | nM | Ki | Eur J Med Chem (2018) 147: 102-114 [PMID:29425815] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting method | B | 7.7 | pKi | 20 | nM | Ki | Medchemcomm (2018) 9: 1033-1044 [PMID:30108992] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A expressed in human HEK293 cells assessed as inhibitory constant incubated for 1 hr by radioligand binding assay | B | 7.7 | pKi | 20 | nM | Ki | Eur J Med Chem (2019) 178: 740-751 [PMID:31229876] |
| ChEMBL | Affinity for 5HT1A receptor | B | 7.77 | pKi | 17 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 3406-3410 [PMID:16677812] |
| ChEMBL | Binding affinity against human 5-hydroxytryptamine 1A receptor | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor | B | 7.82 | pKi | 15 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 1159-1163 [PMID:19147349] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells after 1 hr | B | 7.92 | pKi | 12 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4419-4423 [PMID:23787101] |
| GtoPdb | - | - | 8 | pKi | - | - | - |
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] |
| ChEMBL | Agonist activity at 5HT1A receptor (unknown origin) | F | 8.05 | pKi | 8.9 | nM | Ki | Eur J Med Chem (2018) 145: 74-85 [PMID:29324345] |
| ChEMBL | Binding affinity of compound towards 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT (0.5 nM) ligand in hippocampus + frontal bovine was determined | B | 8.07 | pKi | 8.6 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Ability to displace [3H]-DPAT from 5-hydroxytryptamine 1A receptor in homogenates of bovine hippocampus. | B | 8.18 | pKi | 6.6 | nM | Ki | J Med Chem (1992) 35: 1076-1092 [PMID:1348089] |
| ChEMBL | Displacement of [3H]-8-OH-DAPT from human 5-HT1A receptor expressed in CHO-K1 cells membrane by scintillation counter analysis | B | 8.3 | pKi | 5.01 | nM | Ki | Eur J Med Chem (2022) 233: 114218-114218 [PMID:35248836] |
| 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 | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| 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 | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (2019) 62: 2750-2771 [PMID:30721053] |
| 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 | 8.3 | pKi | 5 | nM | Ki | US-10562853-B2. Compounds for treating disorders sensitive to serotoninergic regulation controlled by the 5-HT1A receptors (2020) |
| ChEMBL | Binding affinity to 5-HT1A (unknown origin) | B | 8.32 | pKi | 4.78 | nM | Ki | J Med Chem (2018) 61: 2166-2210 [PMID:28850227] |
| ChEMBL | Binding affinity to 5HT1A receptor (unknown origin) | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem Lett (2019) 29: 126667-126667 [PMID:31547945] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor of bovine hippocampus. | B | 8.51 | pKi | 3.1 | nM | Ki | J Med Chem (1993) 36: 2066-2074 [PMID:8101876] |
| ChEMBL | In vitro binding affinity against 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT in human CYP3A4 assay | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1709-1712 [PMID:15026055] |
| 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 | 6.73 | pEC50 | 186.21 | nM | EC50 | J Med Chem (2019) 62: 2750-2771 [PMID:30721053] |
| 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 | 6.73 | pEC50 | 186.21 | nM | EC50 | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| ChEMBL | Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay | F | 7.1 | pEC50 | 80 | nM | EC50 | J Med Chem (2006) 49: 3116-3135 [PMID:16722631] |
| 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 | 7.14 | pEC50 | 72.44 | nM | EC50 | J Med Chem (2019) 62: 2750-2771 [PMID:30721053] |
| 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 | 7.14 | pEC50 | 72.44 | nM | EC50 | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| ChEMBL | Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR | F | 7.39 | pEC50 | 41 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 1159-1163 [PMID:19147349] |
| 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 | 7.42 | pEC50 | 38.02 | 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 | 7.82 | pEC50 | 15.14 | nM | EC50 | J Med Chem (2019) 62: 2750-2771 [PMID:30721053] |
| 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 | 7.82 | pEC50 | 15.14 | nM | EC50 | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Binding affinity for 5-hydroxytryptamine 1A receptor with [3H]5-HT | B | 7.34 | pKi | 46.1 | nM | Ki | J Med Chem (1994) 37: 105-112 [PMID:8289183] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat hippocampal membrane | B | 7.44 | pKi | 36 | nM | Ki | Eur J Med Chem (2009) 44: 800-808 [PMID:18603331] |
| ChEMBL | Binding was determined on 5-hydroxytryptamine 1A receptor in rat hippocampal membranes | B | 7.49 | pKi | 32 | nM | Ki | J Med Chem (2001) 44: 4431-4442 [PMID:11728188] |
| ChEMBL | Binding affinity towards rat 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT radioligand. | B | 7.69 | pKi | 20.5 | nM | Ki | J Med Chem (1996) 39: 4439-4450 [PMID:8893838] |
| ChEMBL | Binding affinity at 5-hydroxytryptamine 1A receptor in rat cerebral cortex membranes by [3H]8-OH-DPAT displacement. | B | 7.69 | pKi | 20.5 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 689-694 |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from 5-HT1AR in rat hippocampus | B | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem (2015) 23: 212-221 [PMID:25435254] |
| ChEMBL | Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement | B | 7.7 | pKi | 19.95 | nM | Ki | J Med Chem (1996) 39: 126-134 [PMID:8568799] |
| ChEMBL | In vitro ability to displace [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor sites of rat brain cortex. | B | 7.81 | pKi | 15.4 | nM | Ki | J Med Chem (1995) 38: 1273-1277 [PMID:7731013] |
| ChEMBL | Binding affinity against rat hippocampal 5-hydroxytryptamine 1A (5-HT1A) receptor determined using [3H]8-OH-DPAT as radioligand | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (1996) 39: 4036-4043 [PMID:8831769] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2008) 51: 4529-4538 [PMID:18598015] |
| ChEMBL | Binding affinity by measuring displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor in rat hippocampus | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (1993) 36: 3526-3532 [PMID:7902439] |
| ChEMBL | Evaluated for binding affinity towards 5-hydroxytryptamine 1A receptor in rat brain | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (1988) 31: 1968-1971 [PMID:3172131] |
| ChEMBL | In vitro ability to inhibit binding of radioligand [3H]8-OH-DPAT to 5-hydroxytryptamine 1A receptor in rat cerebral cortex | B | 7.83 | pKi | 14.79 | nM | Ki | J Med Chem (1994) 37: 99-104 [PMID:8289207] |
| ChEMBL | Inhibitory affinity constant against 5-hydroxytryptamine 1A receptor | B | 7.86 | pKi | 13.8 | nM | Ki | J Med Chem (1995) 38: 1701-1710 [PMID:7752194] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor in the rat brain (hippocampus) using [3H]8-OH-DPAT | B | 7.91 | pKi | 12.3 | nM | Ki | J Med Chem (1996) 39: 1125-1129 [PMID:8676348] |
| ChEMBL | In vitro inhibition of [3H]spiperone binding to 5-hydroxytryptamine 1A receptor from rat hippocampal tissue. | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1988) 31: 1382-1392 [PMID:2898533] |
| ChEMBL | In vitro ability to inhibit [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor of rat hippocampus | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1989) 32: 1024-1033 [PMID:2565399] |
| ChEMBL | Antagonist activity against rat hippocampal tissue 5-hydroxytryptamine 1A receptor | F | 8 | pKi | 10 | nM | Ki | J Med Chem (1999) 42: 5077-5094 [PMID:10602693] |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) | B | 8.03 | pKi | 9.31 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Binding affinity against rat 5-hydroxytryptamine 1A receptor | B | 8.03 | pKi | 9.3 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor of rat hippocampal membranes | B | 8.15 | pKi | 7 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 from rat hippocampus | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (1992) 35: 552-558 [PMID:1346653] |
| ChEMBL | Binding affinity was determined against 5-hydroxytryptamine 1A receptor using [3H]WB-4101 | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (1995) 38: 4198-4210 [PMID:7473547] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat hippocampal membranes | B | 8.42 | pKi | 3.8 | nM | Ki | Eur J Med Chem (2009) 44: 152-164 [PMID:18486277] |
| ChEMBL | Binding affinity to 5-hydroxytryptamine 1A receptor in rat hippocampus membranes,3H-8-OH-DPAT and buspirone for nonspecific binding (NSB) | B | 7.22 | pIC50 | 60 | 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 | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (1994) 37: 1779-1793 [PMID:7912735] |
| ChEMBL | Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus | F | 7.28 | pIC50 | 52 | nM | IC50 | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | In vitro inhibition of [3H]8-OH-DPAT binding to rat 5-HT 1a receptors. | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (1999) 42: 490-496 [PMID:9986719] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1A receptor in rat hippocampus membranes using [3H]8-OH-DPAT as radioligand | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1996) 39: 3195-3202 [PMID:8759642] |
| ChEMBL | Binding affinity towards rat 5-hydroxytryptamine 1A receptor was evaluated using [3H]8-OH-DPAT as radioligand | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1996) 39: 4928-4934 [PMID:8960552] |
| ChEMBL | In vitro binding affinity towards the 5-hydroxytryptamine 1A receptor was evaluated | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (1993) 36: 1509-1510 [PMID:8496920] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand. | B | 7.66 | pIC50 | 21.88 | nM | IC50 | J Med Chem (1988) 31: 1087-1093 [PMID:3373482] |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) | B | 7.8 | pIC50 | 16 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | In vitro binding affinity measured on serotonin 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand. | B | 7.89 | pIC50 | 12.8 | nM | IC50 | J Med Chem (1995) 38: 942-949 [PMID:7699710] |
| ChEMBL | In vitro ability to inhibit binding of radioligand [3H]8-OH-DPAT to 5-hydroxytryptamine 1A receptor in rat cerebral cortex | B | 7.89 | pIC50 | 12.8 | nM | IC50 | J Med Chem (1994) 37: 99-104 [PMID:8289207] |
| ChEMBL | Binding affinity to 5-hydroxytryptamine 1A receptor of rat hippocampus with [3H]8-OH-DPAT as radioligand | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 595-598 [PMID:11229779] |
| ChEMBL | Inhibitory concentration against 5-hydroxytryptamine 1A receptor in rat hippocampus membrane using [3H]-8-OH-DPAT as radioligand | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2990-2993 [PMID:15914001] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor using receptor binding assay | B | 8.15 | pIC50 | 7.13 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 2857-2862 |
| 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
| ChEMBL | Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (1994) 37: 105-112 [PMID:8289183] |
| ChEMBL | Binding affinity towards 5-HT1B was determined | B | 4.59 | pIC50 | 26000 | nM | IC50 | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| 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 | 4.9 | pIC50 | 12589.25 | nM | IC50 | J Med Chem (1988) 31: 1087-1093 [PMID:3373482] |
| 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Binding affinity to 5-HT2A (unknown origin) | B | 5.49 | pKi | 3240 | nM | Ki | J Med Chem (2018) 61: 2166-2210 [PMID:28850227] |
| ChEMBL | Displacement of [3H]ketanserin from 5HT2A receptor | B | 6.07 | pKi | 851 | nM | Ki | Eur J Med Chem (2009) 44: 152-164 [PMID:18486277] |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 6.19 | pKi | 653 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 5.64 | pIC50 | 2286 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 5-hydroxytryptamine receptor 2A in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 2 receptor | B | 6.75 | pKi | 178 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortex | B | 5 | pIC50 | 10000 | 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 | Compound was evaluated for binding affinity against 5-hydroxytryptamine 2A receptor using [3H]ketanserin as a radioligand | B | 6.32 | pKi | 482 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 689-694 |
| ChEMBL | Compound was evaluated for the binding affinity towards 5-hydroxytryptamine 2A receptor using [3H]-ketanserin radioligand. | B | 6.32 | pKi | 482 | nM | Ki | J Med Chem (1996) 39: 4439-4450 [PMID:8893838] |
| 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] |
| 5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 6.32 | pKi | 477 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 6.12 | pIC50 | 750 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 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 | 5.64 | pKi | 2270 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
| ChEMBL | In vitro binding affinity towards the 5-hydroxytryptamine 1C receptor at 10 e-6 M | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (1993) 36: 1509-1510 [PMID:8496920] |
| 5-HT3A/5-hydroxytryptamine receptor 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
| ChEMBL | Displacement of [3H]granisetron from human 5HT3A receptor expressed in HEK293 cells by filter binding assay | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2011) 54: 3206-3221 [PMID:21486038] |
| 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting method | B | 6.08 | pKi | 840 | nM | Ki | Bioorg Med Chem (2020) 28: 115262-115262 [PMID:31882369] |
| 5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304] | ||||||||
| GtoPdb | - | - | 6.4 | pKi | - | - | - | Mol Pharmacol (1993) 44: 229-36 [PMID:8394987] |
| 5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
| GtoPdb | - | - | 6.4 | pKi | - | - | - | 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 | 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 | 5.3 | pKi | >5000 | nM | Ki | US-10562853-B2. Compounds for treating disorders sensitive to serotoninergic regulation controlled by the 5-HT1A receptors (2020) |
| 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 | 4.8 | pIC50 | 16000 | 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 | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 5.85 | pKi | 1410 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 5.46 | pIC50 | 3482 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| α1D-adrenoceptor/Alpha-1D adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.28 | pKi | 529 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 5.97 | pIC50 | 1077 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 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 | 5 | pIC50 | 10000 | 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 | 5.21 | pKi | 6100 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Binding affinity towards dopamine receptor D1 in calf striatum | B | 4.57 | pIC50 | 27000 | nM | IC50 | J Med Chem (1994) 37: 1779-1793 [PMID:7912735] |
| 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] |
| D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Binding affinity against Dopamine receptor D2 | B | 6 | pKi | 1000 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Displacement of [3H]methylspiperone from human D2 receptor expressed in HEK cells | B | 6.32 | pKi | 484 | nM | Ki | J Med Chem (2018) 61: 2166-2210 [PMID:28850227] |
| ChEMBL | Displacement of [3H]methylspiperone from human D2 receptor expressed in HEK-GIRK-M4 cell membrane by radioligand binding assay | B | 6.32 | pKi | 484 | nM | Ki | Bioorg Med Chem Lett (2019) 29: 126667-126667 [PMID:31547945] |
| 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 | 6.62 | pKi | 240 | nM | Ki | US-10562853-B2. Compounds for treating disorders sensitive to serotoninergic regulation controlled by the 5-HT1A receptors (2020) |
| ChEMBL | DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) | B | 6.97 | pKi | 108 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Binding affinity for DA2 receptor | B | 7.05 | pKi | 90 | nM | Ki | J Med Chem (1993) 36: 3526-3532 [PMID:7902439] |
| ChEMBL | Displacement of [3H]U-86170 from human D2-dopamine receptor expressed in CHO K1 cells | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (1993) 36: 2066-2074 [PMID:8101876] |
| ChEMBL | Binding affinity to D2 receptor by radioligand binding assay | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (2006) 49: 3116-3135 [PMID:16722631] |
| ChEMBL | DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) | B | 6.49 | pIC50 | 323 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 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 | 7.36 | pKi | 44 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | Displacement of [3H]SDZ-205-501 from Dopamine receptor D2 in calf caudate nucleus. | B | 5.4 | pIC50 | 4000 | nM | IC50 | J Med Chem (1996) 39: 4285-4298 [PMID:8863806] |
| ChEMBL | Binding affinity against D2 receptor in calf caudate nucleus | B | 5.4 | pIC50 | 4000 | 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 towards dopamine receptor D2 using [3H]-raclopride radioligand. | B | 6.07 | pKi | 852 | nM | Ki | J Med Chem (1996) 39: 4439-4450 [PMID:8893838] |
| ChEMBL | Compound was evaluated for binding affinity against Dopamine receptor D2 using [3H]raclopride as a radioligand | B | 6.07 | pKi | 852 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 689-694 |
| ChEMBL | Binding affinity was determined against Dopamine receptor D2 using [3H]spiperone | B | 6.44 | pKi | 367 | nM | Ki | J Med Chem (1995) 38: 4198-4210 [PMID:7473547] |
| ChEMBL | Binding affinity towards dopamine receptor D2 by displacing [3H]spiperone radioligand in rat striatum | B | 6.44 | pKi | 367 | nM | Ki | J Med Chem (1992) 35: 552-558 [PMID:1346653] |
| ChEMBL | In vitro inhibition of [3H]spiperone binding to Dopamine receptor D2 from rat brain limbic tissue | B | 6.92 | pKi | 119 | nM | Ki | J Med Chem (1988) 31: 1382-1392 [PMID:2898533] |
| ChEMBL | In vitro ability to inhibit [3H]spiperone binding to dopamine receptor D2 of rat limbic structures | B | 6.92 | pKi | 119 | nM | Ki | J Med Chem (1989) 32: 1024-1033 [PMID:2565399] |
| ChEMBL | Inhibitory activity against rat limbic tissue Dopamine receptor D2 | B | 6.92 | pKi | 119 | nM | Ki | J Med Chem (1999) 42: 5077-5094 [PMID:10602693] |
| ChEMBL | In vitro ability to inhibit binding of radioligand [3H]spiroperidol to dopamine D2 receptor in rat striatal membrane | B | 7.38 | pKi | 41.69 | nM | Ki | J Med Chem (1994) 37: 99-104 [PMID:8289207] |
| ChEMBL | Binding affinity against Dopamine receptor D2 in rat striatal membrane using [3H]spiroperidol as radioligand | B | 6.55 | pIC50 | 280 | 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 | 6.55 | pIC50 | 280 | nM | IC50 | J Med Chem (1996) 39: 4928-4934 [PMID:8960552] |
| ChEMBL | In vitro binding affinity towards the dopamine receptor D2 at 10 e-6 M | B | 6.58 | pIC50 | 265 | nM | IC50 | J Med Chem (1993) 36: 1509-1510 [PMID:8496920] |
| ChEMBL | In vitro binding affinity measured on dopamine receptor D2 using [3H]spiroperidol as radioligand. | B | 6.65 | pIC50 | 226 | nM | IC50 | J Med Chem (1995) 38: 942-949 [PMID:7699710] |
| ChEMBL | Inhibition of binding of radioligand [3H]spiroperidol to dopamine D2 receptor in rat striatal membranes | B | 6.65 | pIC50 | 222 | nM | IC50 | J Med Chem (1994) 37: 99-104 [PMID:8289207] |
| ChEMBL | Binding affinity to Dopamine receptor D2 in of rat striatum membrane with [3H]- raclopride as radioligand | B | 7.26 | pIC50 | 55 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 595-598 [PMID:11229779] |
| ChEMBL | Inhibitory concentration against Dopamine receptor D2 in rat striatum membrane using [3H]raclopride as radioligand | B | 7.26 | pIC50 | 55 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2990-2993 [PMID:15914001] |
| 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 | 6.18 | pKi | 660 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 7.82 | pKi | 15 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 7.36 | pIC50 | 44 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8] | ||||||||
| ChEMBL | Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| MATE2/Multidrug and toxin extrusion protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8] | ||||||||
| ChEMBL | Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 4.34 | pIC50 | 46000 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| 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] |
| ChEMBL | DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) | B | 6.67 | pKi | 212 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) | B | 6.3 | pIC50 | 504 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | In vitro binding affinity measured on sigma opioid receptor using [3H]DTG as radioligand | B | 6.58 | pIC50 | 263 | nM | IC50 | J Med Chem (1995) 38: 942-949 [PMID:7699710] |
| ChEMBL | The compound was tested for affinity towards sigma-3 receptor | B | 7.44 | pIC50 | 36.31 | nM | IC50 | J Med Chem (1994) 37: 4109-4117 [PMID:7990111] |
| 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 | 7.32 | pKi | 48 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| SERT/Sodium-dependent serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Inhibition of SERT-mediated [3H]5HT uptake in rat synaptosomes by scintillation counting | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2011) 54: 3206-3221 [PMID:21486038] |
| Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244] | ||||||||
| ChEMBL | Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 5.4 | pIC50 | 3981.07 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
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]
