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

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ChEMBL ligand: CHEMBL300555 (NSC-665322, R 5188, R-5188, Spiroxamide, Spiroxatrine)
  • 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];
Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
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];
Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913]
GtoPdb - - 7.3 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470];
Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877]
α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
GtoPdb - - 8.8 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470];
Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877]
α2C-adrenoceptor in Human [GtoPdb: 27] [UniProtKB: P18825]
GtoPdb - - 9 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470];
Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877]

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]