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

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ChEMBL ligand: CHEMBL243954
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT2A receptor in Human [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-HT7 receptor in Human [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
  • Serotonin 7 (5-HT7) receptor in Guinea pig [ChEMBL: CHEMBL5494] [UniProtKB: P50407]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D2 receptor/Dopamine D2 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]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor 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/Serotonin 2a (5-HT2a) receptor 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/Serotonin 7 (5-HT7) receptor 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]
Serotonin 7 (5-HT7) receptor 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]

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]