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

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ChEMBL ligand: CHEMBL225284
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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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/5-hydroxytryptamine receptor 7 in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
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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 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]
ChEMBL Binding affinity to human 5-HT1A receptor extracted from HEK293 cell membrane assessed as inhibition of [3H]-OH-DPAT binding to 5-HT1A by measuring inhibition constant at 1 uM incubated for 1 hrs by microbeta2 reader B 9.66 pKi 0.22 nM Ki Bioorg Med Chem (2024) 104: 117698-117698 [PMID:38552597]
5-HT1A receptor/5-hydroxytryptamine receptor 1A 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/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 Wistar Han rat cortex membranes B 6.49 pKi 326 nM Ki J Med Chem (2004) 47: 6616-6624 [PMID:15588097]
5-HT7 receptor/5-hydroxytryptamine receptor 7 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 Binding affinity to human 5-HT7 receptor extracted from HEK293 cell membrane assessed as inhibition of [3H]LSD binding to 5-HT7 by measuring inhibition constant at 1 uM incubated for 1 hrs by microbeta2 reader B 7.28 pKi 52.7 nM Ki Bioorg Med Chem (2024) 104: 117698-117698 [PMID:38552597]
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/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 9.66 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]
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 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]

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]