LP-12 [Ligand Id: 8434] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL243954
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT7 receptor in Human [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
  • 5-hydroxytryptamine receptor 7 in Guinea pig [ChEMBL: CHEMBL5494] [UniProtKB: P50407]
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  • D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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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 Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HEK293 cells B 7.22 pKi 60.9 nM Ki J Med Chem (2007) 50: 4214-4221 [PMID:17649988]
GtoPdb - - 7.22 pKi 60.9 nM Ki J Med Chem (2007) 50: 4214-21 [PMID:17649988]
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 5.83 pKi 1464 nM Ki J Med Chem (2007) 50: 4214-21 [PMID:17649988]
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Displacement of [3H]ketanserin from 5HT2A receptor in Sprague-Dawley cortex membrane B 5.83 pKi 1464 nM Ki J Med Chem (2007) 50: 4214-4221 [PMID:17649988]
5-HT7 receptor in Human [GtoPdb: 12] [UniProtKB: P34969]
GtoPdb - - 9.89 pKi 0.13 nM Ki J Med Chem (2007) 50: 4214-21 [PMID:17649988]
5-HT7 receptor/5-hydroxytryptamine receptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
ChEMBL Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells B 9.89 pKi 0.13 nM Ki J Med Chem (2007) 50: 4214-4221 [PMID:17649988]
5-hydroxytryptamine receptor 7 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5494] [UniProtKB: P50407]
ChEMBL Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction F 5.75 pEC50 1770 nM EC50 J Med Chem (2007) 50: 4214-4221 [PMID:17649988]
D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Displacement of [3H]spiroperidol from human recombinant Dopamine D2 long receptor B 6.65 pKi 224 nM Ki J Med Chem (2007) 50: 4214-4221 [PMID:17649988]
GtoPdb - - 6.65 pKi 224 nM Ki J Med Chem (2007) 50: 4214-21 [PMID:17649988]

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]