spiroxatrine [Ligand Id: 53] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL300555 (Spiroxatrine, Spiroxamide, R 5188)
  • 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 Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
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  • α1A-adrenoceptor in Human [GtoPdb: 22] [UniProtKB: P35348]
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  • α1B-adrenoceptor in Human [GtoPdb: 23] [UniProtKB: P35368]
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  • α1D-adrenoceptor in Human [GtoPdb: 24] [UniProtKB: P25100]
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  • α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor in Human [GtoPdb: 27] [UniProtKB: P18825]
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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 Binding affinity against Dopamine receptor D2 of rat was determined using 2 nM of [3H]sulpiride in binding assay B 8.84 pKi 1.45 nM Ki J. Med. Chem. (1988) 31: 1965-1968 [PMID:2902227]
ChEMBL Binding affinity against Dopamine receptor D2 of rat was determined using 2 nM of [3H]sulpiride in binding assay B 9.66 pKi 0.22 nM Ki J. Med. Chem. (1988) 31: 1965-1968 [PMID:2902227]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity to 5HT1A receptor B 8.6 pKd 2.51 nM Kd J. Med. Chem. (2009) 52: 6107-6125 [PMID:19754201]
GtoPdb - - 8.8 pKi - - - Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity against 5-hydroxytryptamine 1A receptor of rat was determined using [3H]8-OH-DPAT in binding assay B 7.68 pKi 21 nM Ki J. Med. Chem. (1988) 31: 1965-1968 [PMID:2902227]
ChEMBL Binding affinity against 5-hydroxytryptamine 1A receptor of rat was determined using [3H]8-OH-DPAT in binding assay B 8.72 pKi 1.9 nM Ki J. Med. Chem. (1988) 31: 1965-1968 [PMID:2902227]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1B receptor in rat was determined using 50 uL of [125I]ICYP in binding assay B 5 pKi >10000 nM Ki J. Med. Chem. (1988) 31: 1965-1968 [PMID:2902227]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1B receptor in rat was determined using 50 uL of [125I]ICYP in binding assay B 5 pKi >10000 nM Ki J. Med. Chem. (1988) 31: 1965-1968 [PMID:2902227]
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb - - 6.8 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 17-24 [PMID:9459568]
α1A-adrenoceptor in Human [GtoPdb: 22] [UniProtKB: P35348]
GtoPdb - - 7.3 pKi - - - Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]
α1B-adrenoceptor in Human [GtoPdb: 23] [UniProtKB: P35368]
GtoPdb - - 7.6 pKi - - - Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]
α1D-adrenoceptor in Human [GtoPdb: 24] [UniProtKB: P25100]
GtoPdb - - 7.9 pKi - - - Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]
α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913]
GtoPdb - - 7.3 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470]
α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
GtoPdb - - 8.8 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470]
α2C-adrenoceptor in Human [GtoPdb: 27] [UniProtKB: P18825]
GtoPdb - - 9 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470]

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]