1-phenylbiguanide [Ligand Id: 2284] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL13791 (1-Phenylbiguanide, N-Phenylimidodicarbonimidic Diamide, Phenyl Biguanide)
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  • 5-HT3AB in Human [GtoPdb: 378]
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  • 5-HT3A in Human [GtoPdb: 379]
  • 5-HT3A in Mouse [GtoPdb: 379]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 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 HB3 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094132] [GtoPdb: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8]
ChEMBL Compound was tested for the inhibition of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor expressed in NG 108-15 cells B 5.92 pKi 1200 nM Ki J Med Chem (1996) 39: 4017-4026 [PMID:8831767]
ChEMBL Binding affinity to 5-HT3 serotonin receptor in NG 108-15 neuroblastoma glioma cells using [3H]GR-65630 radioligand. B 5.92 pKi 1200 nM Ki Bioorg Med Chem Lett (2001) 11: 1599-1603 [PMID:11412989]
ChEMBL Binding affinity towards 5-hydroxytryptamine 3 receptor B 5.92 pKi 1200 nM Ki Bioorg Med Chem Lett (2002) 12: 2743-2747 [PMID:12217367]
TAAR5/Trace amine-associated receptor 5 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3784908] [GtoPdb: 170] [UniProtKB: Q5QD14]
ChEMBL Agonist activity at mouse TAAR5 expressed in HEK293 cells assessed as cAMP accumulation after 20 mins by BRET assay F 5 pEC50 >10000 nM EC50 Eur J Med Chem (2017) 127: 781-792 [PMID:27823885]
5-HT3AB in Human [GtoPdb: 378]
GtoPdb - - 4.9 pKi - - - Neuropharmacology (2001) 41: 282-4 [PMID:11489465]
5-HT3A in Human [GtoPdb: 379]
GtoPdb - - 5.6 pKi - - - Mol Pharmacol (1995) 48: 407-16 [PMID:7565620];
Mol Pharmacol (1998) 53: 202-12 [PMID:9463477];
Neuropharmacology (2001) 41: 282-4 [PMID:11489465];
J Neurochem (1995) 65: 104-10 [PMID:7790853];
Br J Pharmacol (1996) 118: 1237-45 [PMID:8818349]
GtoPdb - - 4.1 pEC50 80000 nM EC50 Mol Pharmacol (1995) 48: 1054-62 [PMID:8848005]
5-HT3A in Mouse [GtoPdb: 379]
GtoPdb - - 6.2 pKi - - - J Neurochem (1995) 65: 104-10 [PMID:7790853]
GtoPdb - - 4.5 pEC50 - - - Neuropharmacology (1994) 33: 473-82 [PMID:7984286]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]