EMD-386088 [Ligand Id: 8428] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL364005
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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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-hydroxytryptamine receptor 4 in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
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  • 5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 1A receptor in rat B 6.18 pIC50 660 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 1B receptor in calf B 6.96 pIC50 110 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
5-HT1B receptor/5-hydroxytryptamine receptor 1B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 1B receptor in rat B 6.74 pIC50 180 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 2A receptor in human B 6.62 pIC50 240 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 2C receptor in human B 6.35 pIC50 450 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
5-HT3A/5-hydroxytryptamine receptor 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 3 receptor expressed in NG 108 cells B 7.47 pIC50 34 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
5-hydroxytryptamine receptor 4 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig B 6.21 pIC50 620 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
GtoPdb - - 8.13 pIC50 7.4 nM IC50 Bioorg Med Chem Lett (2005) 15: 4230-4 [PMID:16055331]
ChEMBL Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells B 8.13 pIC50 7.4 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 6 receptor in human B 8.13 pIC50 7.4 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]
ChEMBL Partial agonist activity at 5-HT6 receptor (unknown origin) F 9 pEC50 1 nM EC50 J Med Chem (2024) 67: 1580-1610 [PMID:38190615]
5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 7 receptor in human B 5.52 pIC50 3000 nM IC50 Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331]

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]