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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| 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 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]
