SB 224289 [Ligand Id: 130] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL281350 (SB-224289)
  • 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 Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Mouse [ChEMBL: CHEMBL2405] [GtoPdb: 26] [UniProtKB: P30545]
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  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
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  • FPR1/Formyl peptide receptor 1 in Human [ChEMBL: CHEMBL3359] [GtoPdb: 222] [UniProtKB: P21462]
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  • GPR183/G-protein coupled receptor 183 in Human [ChEMBL: CHEMBL3259470] [GtoPdb: 81] [UniProtKB: P32249]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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  • FPR3/N-formyl peptide receptor 3 in Human [ChEMBL: CHEMBL5646] [GtoPdb: 224] [UniProtKB: P25089]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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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/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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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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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
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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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL Compound was tested for binding affinity against Alpha-1A adrenergic receptor (rat submaxillary gland) B 6 pKi >1000 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL Compound was tested for binding affinity against Alpha-1B adrenergic receptor (rat liver, [3H] prazosin) B 6 pKi >1000 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL PDSP Secondary Binding target: ADRA1D - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 5.68 pKi 2106.2 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL PDSP Secondary Binding target: ADRA2A - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 5.61 pKi 2431.08 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
ChEMBL Compound was tested for binding affinity against human cloned Alpha-2A adrenergic receptor B 6 pKi >1000 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL PDSP Secondary Binding target: ADRA2B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 5.66 pKi 2172.45 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2405] [GtoPdb: 26] [UniProtKB: P30545]
ChEMBL Compound was tested for binding affinity against Alpha-2B adrenergic receptor (NG 108-15 cells) using [3H]RX-821002) as radioligand B 6 pKi >1000 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
apelin receptor/Apelin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1628481] [GtoPdb: 36] [UniProtKB: P35414]
ChEMBL GPCR PRESTO-Tango dose-response in antagonist mode with target: APLNR F 5.44 pIC50 3632.38 nM IC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL Compound was tested for binding affinity against human cloned Beta-1 adrenergic receptor B 6 pKi >1000 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL Compound was tested for binding affinity against human cloned Beta-2 adrenergic receptor B 6 pKi >1000 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL PDSP Secondary Binding target: DRD1 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 6.43 pKi 369.36 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Compound was tested for binding affinity against human cloned Dopamine receptor D2 B 6 pKi >1000 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Compound was tested for binding affinity against human cloned Dopamine receptor D3 B 6 pKi >1000 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
ChEMBL PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 5.97 pKi 1077.83 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL PDSP Secondary Binding target: SLC6A3 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 5.93 pKi 1180.59 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
FPR1/Formyl peptide receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3359] [GtoPdb: 222] [UniProtKB: P21462]
ChEMBL GPCR PRESTO-Tango dose-response in antagonist mode with target: FPR1 F 5.37 pIC50 4245.51 nM IC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
GPR183/G-protein coupled receptor 183 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3259470] [GtoPdb: 81] [UniProtKB: P32249]
ChEMBL GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183 F 5.19 pIC50 6498.97 nM IC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
GPR35/G-protein coupled receptor 35 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293267] [GtoPdb: 102] [UniProtKB: Q9HC97]
ChEMBL GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR35 F 5.34 pIC50 4581.88 nM IC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL Compound was tested for binding affinity against Histamine H1 receptor. B 6 pKi >1000 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
Histamine H2 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2882] [UniProtKB: P47747]
ChEMBL Compound was tested for binding affinity towards Histamine H2 receptor B 6 pKi >1000 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL PDSP Secondary Binding target: CHRM1 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 5.9 pKi 1263.86 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
ChEMBL Compound was tested for binding affinity against human cloned Muscarinic acetylcholine receptor M1 B 6 pKi >1000 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Compound was tested for binding affinity against human cloned Muscarinic acetylcholine receptor M2 B 6 pKi >1000 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
ChEMBL GPCR PRESTO-Tango dose-response in antagonist mode with target: CHRM2 F 5.47 pIC50 3422.5 nM IC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL PDSP Secondary Binding target: CHRM3 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 6.03 pKi 926.08 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL PDSP Secondary Binding target: CHRM5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 6.46 pKi 344 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
FPR3/N-formyl peptide receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5646] [GtoPdb: 224] [UniProtKB: P25089]
ChEMBL GPCR PRESTO-Tango dose-response in antagonist mode with target: FPR3 F 5.42 pIC50 3838.14 nM IC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL PDSP Secondary Binding target: SLC6A2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 5.76 pKi 1729.62 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
GPR65/Psychosine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3714081] [GtoPdb: 113] [UniProtKB: Q8IYL9]
ChEMBL GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR65 F 5.39 pIC50 4057.96 nM IC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Compound was tested for binding affinity against human 5-hydroxytryptamine 1A receptor B 5.5 pKi >3162.28 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
ChEMBL Affinity for 5-hydroxytryptamine 1A receptor subtype B 6 pKi >1000 nM Ki Bioorg Med Chem Lett (1997) 7: 3183-3188
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Inhibition activity against 5-hydroxytryptamine 1A receptor in rat hippocampus membranes using radio binding assays B 6 pIC50 >1000 nM IC50 J Med Chem (2000) 43: 517-525 [PMID:10669578]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Affinity for 5-hydroxytryptamine 1B receptor subtype B 8 pKi 10 nM Ki Bioorg Med Chem Lett (1997) 7: 3183-3188
ChEMBL In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand B 8 pKi 10 nM Ki Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528]
ChEMBL Binding affinity for human 5-hydroxytryptamine 1B receptor B 8.2 pKi 6.31 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
ChEMBL PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 8.56 pKi 2.78 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
GtoPdb - - 8.6 pKi 2.51 nM Ki Br J Pharmacol (1998) 125: 202-8 [PMID:9776361];
Mol Pharmacol (2000) 58: 1042-9 [PMID:11040052];
J Med Chem (1998) 41: 1218-35 [PMID:9548813]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay B 8.7 pIC50 2 nM IC50 J Med Chem (2000) 43: 517-525 [PMID:10669578]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL Binding affinity for human 5-hydroxytryptamine 1D receptor B 6.3 pKi 501.19 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
GtoPdb - - 6.3 pKi - - - Br J Pharmacol (1998) 125: 202-8 [PMID:9776361];
J Med Chem (1998) 41: 1218-35 [PMID:9548813]
ChEMBL PDSP Secondary Binding target: HTR1D - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 6.43 pKi 367.88 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
ChEMBL Affinity for 5-hydroxytryptamine 1D receptor subtype B 6.59 pKi 260 nM Ki Bioorg Med Chem Lett (1997) 7: 3183-3188
ChEMBL Inhibition affinity against 5-HT-1D receptor in bovine caudate nucleus using radio binding assay B 6 pIC50 >1000 nM IC50 J Med Chem (2000) 43: 517-525 [PMID:10669578]
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
ChEMBL Compound was tested for binding affinity against human 5-hydroxytryptamine 1E receptor B 5 pKi >10000 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939]
ChEMBL Compound was tested for binding affinity against human 5-hydroxytryptamine 1F receptor B 5 pKi >10000 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 5.3 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
ChEMBL PDSP Secondary Binding target: HTR2A - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 5.75 pKi 1784.23 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
ChEMBL Binding affinity for human 5-hydroxytryptamine 2A receptor B 5.8 pKi 1584.89 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
GtoPdb - - 5.7 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
ChEMBL PDSP Secondary Binding target: HTR2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 6.07 pKi 859.31 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
ChEMBL Compound was tested for binding affinity against human 5-hydroxytryptamine 2C receptor B 6.2 pKi 630.96 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
GtoPdb - - 6.2 pKi - - - Br J Pharmacol (1998) 125: 202-8 [PMID:9776361]
Serotonin 4 (5-HT4) receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2696] [UniProtKB: Q6Q253]
ChEMBL Compound was tested for binding affinity against piglet hippocampus 5-hydroxytryptamine 4 receptor B 6 pKi >1000 nM Ki J Med Chem (1998) 41: 1218-1235 [PMID:9548813]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL Inhibition of 5-hydroxytryptamine reuptake B 5.33 pIC50 4700 nM IC50 J Med Chem (2000) 43: 517-525 [PMID:10669578]
σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2]
ChEMBL PDSP Secondary Binding target: TMEM97 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 6.3 pKi 502.11 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL PDSP Secondary Binding target: SIGMAR1 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 5.36 pKi 4339.6 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb - - 5.9 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]

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]