LP-44 [Ligand Id: 8435] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL225284
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • 8.14
1 CHEMBL225284_lig_chart_1 Dopamine D2 receptor Human
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
  • 7.28
2 CHEMBL225284_lig_chart_2 Serotonin 1a (5-HT1a) receptor HumanRat
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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]
  • 6.49
3 CHEMBL225284_lig_chart_3 5-HT2A receptor HumanRat
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
  • 9.66
4 CHEMBL225284_lig_chart_4 Serotonin 7 (5-HT7) receptor HumanRat
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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 8.14 pKi 7.3 nM Ki J. Med. Chem. (2007) 50: 4214-4221 [PMID:17649988]
GtoPdb - - 8.14 pKi 7.3 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 5-HT1A receptor expressed in HEK293 cells after 1 hr by beta-counting B 7.28 pKi 52.7 nM Ki Eur. J. Med. Chem. (2014) 78: 10-22 [PMID:24675176]
ChEMBL Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry B 7.28 pKi 52.7 nM Ki Eur. J. Med. Chem. (2014) 85: 716-726 [PMID:25128671]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells after 1 hr B 7.28 pKi 52.7 nM Ki Eur. J. Med. Chem. (2015) 92: 202-211 [PMID:25555143]
GtoPdb - - 7.28 pKi 52.7 nM Ki J Med Chem (2007) 50: 4214-21 [PMID:17649988]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Displacement of [3H]8-OH-DPAT from 5HT1A receptor in Wistar Han rat hippocampal membranes B 7.28 pKi 52.7 nM Ki J. Med. Chem. (2004) 47: 6616-6624 [PMID:15588097]
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 6.49 pKi 326 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 Wistar Han rat cortex membranes B 6.49 pKi 326 nM Ki J. Med. Chem. (2004) 47: 6616-6624 [PMID:15588097]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileum B 7.7 pKd 19.95 nM Kd J. Med. Chem. (2004) 47: 6616-6624 [PMID:15588097]
ChEMBL Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting B 9.66 pKi 0.22 nM Ki Eur. J. Med. Chem. (2014) 78: 10-22 [PMID:24675176]
ChEMBL Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry B 9.66 pKi 0.22 nM Ki Eur. J. Med. Chem. (2014) 85: 716-726 [PMID:25128671]
ChEMBL Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr B 9.66 pKi 0.22 nM Ki Eur. J. Med. Chem. (2015) 92: 202-211 [PMID:25555143]
GtoPdb - - 9.66 pKi 0.22 nM Ki J Med Chem (2007) 50: 4214-21 [PMID:17649988]
ChEMBL Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum F 5.59 pEC50 2560 nM EC50 J. Med. Chem. (2004) 47: 6616-6624 [PMID:15588097]
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 9.66 pKi 0.22 nM Ki J. Med. Chem. (2004) 47: 6616-6624 [PMID:15588097]
ChEMBL Displacement of [3H]LSD from rat cloned 5-Hydroxytryptamine receptor 7 after 60 mins B 9.66 pKi 0.22 nM Ki J. Med. Chem. (2016) 59: 810-840 [PMID:26390077]
ChEMBL Displacement of [3H]LSD from rat recombinant 5-HT7 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assay B 9.66 pKi 0.22 nM Ki J Med Chem (2018) 61: 8475-8503 [PMID:29767995]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]