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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]