buspirone [Ligand Id: 36] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL49 (BCI-024, Buspar, 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 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 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 | 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 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 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 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-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 | 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 | 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
