buspirone [Ligand Id: 36] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL49 (BCI-024, Buspar, Buspirona, Buspirone, Gen-buspirone) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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] |
| Dopamine D1 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/Dopamine D1 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/Dopamine D2 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 | 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 | 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 | 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 | DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) | B | 6.49 | pIC50 | 323 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Dopamine D2 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/Dopamine D2 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/Dopamine D3 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 |
| Kv11.1/HERG 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] |
| 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] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor 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 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 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 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 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 | 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 | Affinity for 5HT1A receptor | B | 7.77 | pKi | 17 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 3406-3410 [PMID:16677812] |
| 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 | 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 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 | 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/Serotonin 1a (5-HT1a) receptor 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/Serotonin 1b (5-HT1b) receptor 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/Serotonin 2a (5-HT2a) receptor 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 |
| Serotonin 2a (5-HT2a) receptor 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/Serotonin 2a (5-HT2a) receptor 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/Serotonin 2b (5-HT2b) receptor 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/Serotonin 2c (5-HT2c) receptor 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/Serotonin 2c (5-HT2c) receptor 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/Serotonin 3a (5-HT3a) receptor 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/Serotonin 7 (5-HT7) receptor 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] |
| SERT/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] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor 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 opioid receptor 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] |
| 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] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
