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

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ChEMBL ligand: CHEMBL294083
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-hydroxytryptamine receptor 4 in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
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  • D2 receptor/D(2) dopamine receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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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 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/5-hydroxytryptamine receptor 2A 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-hydroxytryptamine receptor 4 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]
D2 receptor/D(2) dopamine 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-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]

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]