compound 3 [PMID: 32258933] [Ligand Id: 11214] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL294083
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
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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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL In vitro by displacement of [3H]raclopride from Dopamine receptor D2 on rat striatal membrane B 6 pKi <1000 nM Ki J Med Chem (1997) 40: 586-593 [PMID:9046349]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum NF54 incubated for 48 hrs by lactate dehydrogenase assay F 7.21 pIC50 62 nM IC50 J Med Chem (2023) 66: 8382-8406 [PMID:37357390]
ChEMBL Antiplasmodial activity against Plasmodium falciparum K1 incubated for 48 hrs by lactate dehydrogenase assay F 7.27 pIC50 54 nM IC50 J Med Chem (2023) 66: 8382-8406 [PMID:37357390]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL In vitro by displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor on rat cortical membrane B 6 pKi <1000 nM Ki J Med Chem (1997) 40: 586-593 [PMID:9046349]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Binding affinity was evaluated in vitro by displacement of [3H]ketanserin from 5-hydroxytryptamine 2A receptor on rat cortical membrane B 6 pKi <1000 nM Ki J Med Chem (1997) 40: 586-593 [PMID:9046349]
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16]
ChEMBL In vitro by displacement of [3H]LY-278584 from 5-hydroxytryptamine 3 receptor on rat entorhinal cortex B 9.5 pKi 0.32 nM Ki J Med Chem (1997) 40: 586-593 [PMID:9046349]
ChEMBL Rat 5-hydroxytryptamine 3 receptor (5-HT3) antagonist F 9.5 pKi 0.32 nM Ki J Med Chem (1998) 41: 2029-2039 [PMID:9622544]
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
ChEMBL In vitro by displacement of [3H]GR-113808 from 5-hydroxytryptamine 4 receptor on guinea pig striatal membrane B 6 pKi <1000 nM Ki J Med Chem (1997) 40: 586-593 [PMID:9046349]

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]