buspirone [Ligand Id: 36] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL49 (Buspirone, Buspar, BCI-024)
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
  • This target only has 1 pki data point
  • 5.85
1 CHEMBL49_lig_chart_1 Alpha-1a adrenergic receptor BovineRat
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
  • This target only has 1 pki data point
  • 6.28
2 CHEMBL49_lig_chart_2 Alpha-1d adrenergic receptor Human
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  • Alpha-2a adrenergic receptor in Bovine [ChEMBL: CHEMBL4744] [UniProtKB: Q28838]
  • This target only has 0 pki data point
  • 0
3 CHEMBL49_lig_chart_3 Alpha-2a adrenergic receptor Bovine
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4 CHEMBL49_lig_chart_4 Dopamine D1 receptor BovineMouse
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • Dopamine D2 receptor in Bovine [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
  • 6.68
5 CHEMBL49_lig_chart_5 Dopamine D2 receptor HumanBovineRat
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
  • 7
6 CHEMBL49_lig_chart_6 Dopamine D3 receptor Human
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  • Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
  • This target only has 0 pki data point
  • 0
7 CHEMBL49_lig_chart_7 HERG Human
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  • Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8]
  • This target only has 0 pki data point
  • 0
8 CHEMBL49_lig_chart_8 Multidrug and toxin extrusion protein 1 Human
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  • MATE2/Multidrug and toxin extrusion protein 2 in Human [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8]
  • This target only has 0 pki data point
  • 0
9 CHEMBL49_lig_chart_9 Multidrug and toxin extrusion protein 2 Human
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
  • 7.83
10 CHEMBL49_lig_chart_10 Serotonin 1a (5-HT1a) receptor HumanRat
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
  • This target only has 1 pki data point
  • 7.77
11 CHEMBL49_lig_chart_11 Serotonin 1b (5-HT1b) receptor Rat
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • Serotonin 2a (5-HT2a) receptor in Bovine [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
  • 6.32
12 CHEMBL49_lig_chart_12 Serotonin 2a (5-HT2a) receptor HumanBovineRat
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
  • This target only has 1 pki data point
  • 6.32
13 CHEMBL49_lig_chart_13 Serotonin 2b (5-HT2b) receptor Human
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
  • This target only has 1 pki data point
  • 0
14 CHEMBL49_lig_chart_14 Serotonin 2c (5-HT2c) receptor HumanRat
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  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
  • This target only has 1 pki data point
  • 5
15 CHEMBL49_lig_chart_15 Serotonin 3a (5-HT3a) receptor Human
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  • SERT/Serotonin transporter in Rat [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
  • This target only has 0 pki data point
  • 0
16 CHEMBL49_lig_chart_16 Serotonin transporter Rat
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
  • 7.32
17 CHEMBL49_lig_chart_17 Sigma opioid receptor HumanRat
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  • Organic cation transporter 2/Solute carrier family 22 member 2 in Human [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
  • This target only has 0 pki data point
  • 0
18 CHEMBL49_lig_chart_18 Solute carrier family 22 member 2 Human
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  • 5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
  • 5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
  • 6.4
19 CHEMBL49_lig_chart_19 5-HT7 receptor MouseRat
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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]-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 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]-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]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 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 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 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
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 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 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 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]
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