AL-37350A [Ligand Id: 160] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL133455
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor/5-hydroxytryptamine receptor 1D in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT3A/5-hydroxytryptamine receptor 3A in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
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  • 5-HT4 receptor/5-hydroxytryptamine receptor 4 in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
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  • 5-HT5A receptor/5-hydroxytryptamine receptor 5A in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
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  • 5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • 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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  • 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 Rat [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
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  • α2C-adrenoceptor/Alpha-2C adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • NET/Sodium-dependent noradrenaline transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • SERT/Sodium-dependent serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL In vitro inhibitory concentration required against [3H]8-OH-DPAT binding to cloned human 5-hydroxytryptamine 1A receptor B 5 pIC50 >10000 nM IC50 J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Inhibitory constant against 5-hydroxytryptamine 1B receptor using with [125I]- cyanopindolol radioligand B 5.48 pKi 3300 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
5-HT1D receptor/5-hydroxytryptamine receptor 1D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL Inhibitory constant against human 5-hydroxytryptamine 5A receptor using [3H]LSD radioligand B 5 pKi >10000 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Inhibitory constant against cloned human 5-hydroxytryptamine 2A receptor using with [125I]- DOI radioligand B 8.7 pKi 2 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
GtoPdb - - 8.7 pKi - - - J Med Chem (2003) 46: 4188-95 [PMID:12954071]
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL In vitro inhibitory constant against [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex B 9.7 pKi 0.2 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
ChEMBL In vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex B 9.3 pIC50 0.5 nM IC50 J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
ChEMBL In vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cells F 7.1 pEC50 80.1 nM EC50 J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand B 8.28 pKi 5.3 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
GtoPdb - - 8.3 pKi - - - J Med Chem (2003) 46: 4188-95 [PMID:12954071]
5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Inhibitory constant against cloned human 5-hydroxytryptamine 2C receptor using with [125I]- DOI radioligand B 8.47 pKi 3.4 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
GtoPdb - - 8.5 pKi - - - J Med Chem (2003) 46: 4188-95 [PMID:12954071]
5-HT3A/5-hydroxytryptamine receptor 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Inhibitory constant against 5-hydroxytryptamine 3 receptor using [3H]GR-65630 radioligand B 5 pKi >10000 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
5-HT4 receptor/5-hydroxytryptamine receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
ChEMBL Inhibitory constant against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 radioligand B 5.77 pKi 1700 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
5-HT5A receptor/5-hydroxytryptamine receptor 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
ChEMBL Inhibitory constant against human 5-hydroxytryptamine 1D receptor using [3H]5-CT radioligand B 5 pKi >10000 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Inhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligand B 5.66 pKi 2200 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
α1A-adrenoceptor/Alpha-1A adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL Inhibitory constant against alpha-1A receptor using [3H]-7-MeO prazosin radioligand B 5 pKi >10000 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
α1B-adrenoceptor/Alpha-1B adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL Inhibitory constant against Alpha-1B adrenergic radioligand B 5 pKi >10000 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
α2A-adrenoceptor/Alpha-2A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Inhibitory concentration required against Alpha-2A adrenergic receptor using [3H]clonidine radioligand B 4.72 pIC50 19000 nM IC50 J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
α2B-adrenoceptor/Alpha-2B adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
ChEMBL Inhibitory constant against Alpha-2B adrenergic receptor using [3H]MK-912 radioligand B 5 pKi >10000 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
α2C-adrenoceptor/Alpha-2C adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Inhibitory concentration required against Alpha-2A adrenergic receptor using [3H]clonidine radioligand B 4.85 pIC50 14000 nM IC50 J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
NET/Sodium-dependent noradrenaline transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL Inhibitory constant against norepinephrine transporter receptor using [3H]radioligand B 5 pKi >10000 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]
SERT/Sodium-dependent serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL Inhibitory constant against human serotonin transporter using [3H]N-Me-citalopram radioligand B 5 pKi >10000 nM Ki J Med Chem (2003) 46: 4188-4195 [PMID:12954071]

ChEMBL data shown on this page come from version 36:

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]