spiperone [Ligand Id: 99] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL267930 (R 5147, Spiperone, Spiropitan)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
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  • α1D-adrenoceptor in Human [GtoPdb: 24] [UniProtKB: P25100]
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • HLA class I histocompatibility antigen A-3 in Human [ChEMBL: CHEMBL2632] [UniProtKB: P04439]
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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]
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  • 5-HT1B receptor in Mouse [GtoPdb: 2] [UniProtKB: P28334]
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
  • 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
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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]
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  • 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Mouse [ChEMBL: CHEMBL4764] [GtoPdb: 12] [UniProtKB: P32304]
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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  • Vesicular acetylcholine transporter in Rat [ChEMBL: CHEMBL2125] [GtoPdb: 1013] [UniProtKB: Q62666]
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  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
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  • D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active B 8.1 pKi 7.9 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 657-664 [PMID:15664832]
GtoPdb - - 8.3 pKi - - - Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay B 7.87 pKi 13.49 nM Ki J. Med. Chem. (1996) 39: 4602-4607 [PMID:8917649]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay B 7.42 pKi 38.02 nM Ki J. Med. Chem. (1996) 39: 4602-4607 [PMID:8917649]
ChEMBL Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland B 8.14 pKi 7.2 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Compound was tested for binding affinity against cloned Alpha-1B adrenergic receptor from hamster smooth muscle using radioligand ([3H]prazosin) binding assay B 8.15 pKi 7.08 nM Ki J. Med. Chem. (1996) 39: 4602-4607 [PMID:8917649]
GtoPdb - - 9.2 pKi - - - Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL Overall binding displacement in tissues containing only the Alpha-1B adrenergic receptor (rat spleen, rat liver) B 8.89 pKi 1.3 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
α1D-adrenoceptor in Human [GtoPdb: 24] [UniProtKB: P25100]
GtoPdb - - 8.1 pKi - - - Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
ChEMBL Compound was tested for binding affinity against cloned Alpha-1D adrenergic receptor from rat brain. B 7.66 pKi 21.88 nM Ki J. Med. Chem. (1996) 39: 4602-4607 [PMID:8917649]
Beta casein in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2210] [UniProtKB: P02665]
ChEMBL Compound was tested for binding Alpha-1B adrenergic receptor from rat liver using radioligand ([3H]prazosin) binding assay B 8.81 pKi 1.55 nM Ki J. Med. Chem. (1996) 39: 4602-4607 [PMID:8917649]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey B 6.49 pKi 323 nM Ki J. Med. Chem. (1991) 34: 3235-3241 [PMID:1956042]
GtoPdb - - 6.7 pKi - - - Nature (1991) 350: 614-9 [PMID:1826762]
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate B 5.52 pKi >3000 nM Ki J. Med. Chem. (1989) 32: 1431-1435 [PMID:2525621]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Binding affinity to dopamine D2 receptor in human brain caudate nucleus B 9.8 pKd 0.16 nM Kd Bioorg. Med. Chem. (2016) 24: 3671-3679 [PMID:27364609]
ChEMBL Displacement of [3H]spiperone from dopamine D2 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter B 8.92 pKi 1.2 nM Ki Bioorg. Med. Chem. (2013) 21: 856-868 [PMID:23332346]
ChEMBL Displacement of [3H]-spiperone from dopamine D2 receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometry B 8.97 pKi 1.08 nM Ki Bioorg. Med. Chem. Lett. (2015) 25: 3970-3974 [PMID:26227779]
ChEMBL Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells. B 9.3 pKi 0.5 nM Ki US-9359372-B2. Hexahydrodibenzo[a,g]quinolizine compound, preparation method thereof, pharmaceutical composition and use thereof (2016)
ChEMBL Displacement of [3H]spiperone from human dopamine D2 receptor expressed in HEK293 cells B 9.36 pKi 0.44 nM Ki Bioorg. Med. Chem. (2008) 16: 6675-6681 [PMID:18562201]
ChEMBL Displacement of [3H]Spiprone from human dopamine D2 receptor expressed in HEK293 cells B 9.55 pKi 0.28 nM Ki Bioorg. Med. Chem. (2012) 20: 4862-4871 [PMID:22748706]
ChEMBL Tested for binding affinity against dopamine receptor D2 B 9.7 pKi 0.2 nM Ki J. Med. Chem. (1993) 36: 2519-2525 [PMID:8355253]
ChEMBL Binding affinity for human dopamine receptor D2 long B 9.92 pKi 0.12 nM Ki J. Med. Chem. (2005) 48: 694-709 [PMID:15689154]
ChEMBL Displacement of [3H]sulpiride from dopamine D2 receptor B 10 pKi 0.1 nM Ki J. Nat. Prod. (1993) 56: 441-455 [PMID:8496700]
ChEMBL Displacement of [3H]Spiperone from human recombinant dopamine D2S receptor expressed in CHO cells after 2 hrs B 10.05 pKi 0.09 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Binding affinity against dopamine receptor D2 by using [3H]spiperone as radioligand in caudate-putamen of monkey B 10.22 pKi 0.06 nM Ki J. Med. Chem. (1991) 34: 3235-3241 [PMID:1956042]
ChEMBL Displacement of [125I]ABN from human dopamine D2 long receptor expressed in HEK293 cell membranes after 60 mins by scintillation counting method B 10.22 pKi 0.06 nM Ki J Med Chem (2017) 60: 9905-9910 [PMID:29125762]
ChEMBL Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells. B 8.59 pIC50 2.56 nM IC50 US-9359372-B2. Hexahydrodibenzo[a,g]quinolizine compound, preparation method thereof, pharmaceutical composition and use thereof (2016)
ChEMBL Displacement of [3H]Spiprone from human dopamine D2 receptor expressed in HEK293 cells B 8.9 pIC50 1.27 nM IC50 Bioorg. Med. Chem. (2012) 20: 4862-4871 [PMID:22748706]
ChEMBL Displacement of [3H]Spiperone from human recombinant dopamine D2S receptor expressed in CHO cells after 2 hrs B 9.6 pIC50 0.25 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control. B 8.85 pEC50 1.4 nM EC50 US-9359372-B2. Hexahydrodibenzo[a,g]quinolizine compound, preparation method thereof, pharmaceutical composition and use thereof (2016)
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Compound was tested for binding affinity against native Dopamine receptor D2 from rat striatum using radioligand [3H]-spiperone) B 9.24 pKi 0.58 nM Ki J. Med. Chem. (1996) 39: 4602-4607 [PMID:8917649]
ChEMBL Binding affinity against rat Dopamine receptor D2. B 9.3 pKi 0.5 nM Ki J. Med. Chem. (1998) 41: 5084-5093 [PMID:9836624]
ChEMBL Inhibitory constant against dopamine D2 receptor using 0.2 nM [3H]-spiperone B 9.38 pKi 0.42 nM Ki J. Med. Chem. (2005) 48: 266-273 [PMID:15634021]
GtoPdb - - 9.4 pKi - - - Eur J Pharmacol (1994) 266: 79-85 [PMID:7907989];
Nature (1990) 347: 146-51 [PMID:1975644];
J Pharmacol Exp Ther (1995) 275: 885-898 [PMID:7473180];
J Pharmacol Exp Ther (1994) 268: 495-502 [PMID:8301592]
ChEMBL Inhibitory constant against binding of [125I]- IBZM to rat striatal membrane B 9.83 pKi 0.15 nM Ki J. Med. Chem. (1988) 31: 1039-1043 [PMID:2966245]
ChEMBL Displacement of [3H]spiperone from dopamine receptor D2 B 10.24 pKi 0.06 nM Ki J. Med. Chem. (1992) 35: 423-430 [PMID:1531364]
ChEMBL Binding affinity of compound against Dopamine receptor D2 binding site using radioligand [3H]spiperone B 10.35 pKi 0.04 nM Ki J. Med. Chem. (1989) 32: 1959-1962 [PMID:2569041]
ChEMBL Competitive binding assay against Dopamine receptor D2 in rat striatal membranes and [125I]-IBF radioligand B 10.82 pKi 0.01 nM Ki J. Med. Chem. (1990) 33: 171-178 [PMID:2136916]
ChEMBL In vitro inhibition of [3H]spiroperidol binding to rat Dopamine D2 receptors. B 10.22 pIC50 0.06 nM IC50 J. Med. Chem. (1999) 42: 490-496 [PMID:9986719]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL In vitro binding affinity on D3 receptor is inhibition of binding of [125I]- NCQ 298 to Sf9 cells infected with recombinant baculovirus B 8.88 pKi 1.31 nM Ki J. Med. Chem. (1993) 36: 3707-3720 [PMID:8246241]
GtoPdb - - 9.2 pKi - - - Nature (1990) 347: 146-51 [PMID:1975644]
ChEMBL Displacement of [3H]-spiperone from dopamine D3 receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometry B 9.32 pKi 0.48 nM Ki Bioorg. Med. Chem. Lett. (2015) 25: 3970-3974 [PMID:26227779]
ChEMBL Displacement of [125I]ABN from human dopamine D3 receptor expressed in HEK293 cell membranes after 60 mins by scintillation counting method B 9.48 pKi 0.33 nM Ki J Med Chem (2017) 60: 9905-9910 [PMID:29125762]
ChEMBL Displacement of [125I]IABN from recombinant human D3 receptor stably expressed in HEK293 cell membranes measured after 60 mins by scintillation counting analysis B 9.48 pKi 0.33 nM Ki J Med Chem (2019) 62: 5132-5147 [PMID:31021617]
ChEMBL Binding affinity to dopamine D3 receptor (unknown origin) B 9.49 pKi 0.32 nM Ki Bioorg. Med. Chem. (2016) 24: 3671-3679 [PMID:27364609]
ChEMBL Binding affinity for human dopamine receptor D3 B 9.6 pKi 0.25 nM Ki J. Med. Chem. (2005) 48: 694-709 [PMID:15689154]
ChEMBL Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells B 9.6 pKi 0.25 nM Ki J. Med. Chem. (2003) 46: 4377-4392 [PMID:14521403]
ChEMBL Displacement of [3H]Spiperone from human recombinant dopamine D3 receptor expressed in CHO cells after 2 hrs B 9.92 pKi 0.12 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Antagonist activity at dopamine D3 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 assessed as inhibition of agonist-induced response incubated for 60 mins in incubator followed by 15 mins at room temperature by FLIPR assay B 7.01 pIC50 97 nM IC50 J. Med. Chem. (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL Antagonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of dopamine-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay F 7.03 pIC50 93.2 nM IC50 J Med Chem (2018) 61: 10017-10039 [PMID:30383372]
ChEMBL Displacement of [3H]Spiperone from human recombinant dopamine D3 receptor expressed in CHO cells after 2 hrs B 9.44 pIC50 0.36 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Binding affinity to dopamine D4 receptor (unknown origin) B 8.85 pKi 1.4 nM Ki Bioorg. Med. Chem. (2016) 24: 3671-3679 [PMID:27364609]
GtoPdb - - 9.3 pKi - - - Life Sci (1995) 57: PL275-83 [PMID:7475902]
ChEMBL Binding affinity to dopamine D4 receptor (unknown origin) B 9.35 pKi 0.45 nM Ki J Med Chem (2017) 60: 9905-9910 [PMID:29125762]
ChEMBL Inhibition of D4 receptor (unknown origin) B 9.35 pKi 0.45 nM Ki J Med Chem (2019) 62: 5132-5147 [PMID:31021617]
ChEMBL Binding affinity for Dopamine receptor D4 B 9.48 pKi 0.33 nM Ki J. Med. Chem. (2005) 48: 694-709 [PMID:15689154]
ChEMBL Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs B 9.7 pKi 0.2 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs B 9.3 pIC50 0.5 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
HLA class I histocompatibility antigen A-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2632] [UniProtKB: P04439]
ChEMBL Binding affinity to human biotinylated HLA-A2 by surface plasmon resonance assay B 5.6 pKd 2500 nM Kd Bioorg Med Chem Lett (2018) 28: 2837-2841 [PMID:30077568]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL DNDI: Malaria in Vitro, 72 hour F 5.75 pIC50 1760 nM IC50 Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning
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 7.4 pKd 39.81 nM Kd J. Med. Chem. (2009) 52: 6107-6125 [PMID:19754201]
ChEMBL Displacement of [3H]spiperone from human recombinant 5HT1A receptor expressed in CHO cell membrane incubated for 1 hr by scintillation counting method B 7.76 pKi 17.2 nM Ki Bioorg. Med. Chem. (2016) 24: 3671-3679 [PMID:27364609]
GtoPdb - - 8.8 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]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor by the displacement of [125I]trans-8-OH-PIPAT in membrane homogenates of hippocampal tissue of rat brain B 6.22 pKi 602 nM Ki J. Med. Chem. (1993) 36: 3161-3165 [PMID:8230102]
ChEMBL Binding affinity against rat 5-hydroxytryptamine 1A receptor in CHO cells. B 7.24 pKi 58 nM Ki J. Med. Chem. (1998) 41: 5084-5093 [PMID:9836624]
ChEMBL Tested for binding affinity against 5-hydroxytryptamine 1A receptor from rat frontal cortical regions using [3H]8-OH-DPAT as radioligand B 7.31 pKi 49 nM Ki J. Med. Chem. (1993) 36: 2519-2525 [PMID:8355253]
ChEMBL Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand. B 7.4 pKi 40 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
ChEMBL Binding affinity of compound against 5-hydroxytryptamine 1A receptor binding site using radioligand [3H]8-OH-DPAT B 7.52 pKi 30 nM Ki J. Med. Chem. (1989) 32: 1959-1962 [PMID:2569041]
ChEMBL