[3H]meta-chlorophenylbiguanide [Ligand Id: 2304] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL13790 (3-Chloro-Phenyl Biguanide, M-Chlorophenylbiguanidine, N-(3-Chlorophenyl)Imidodicarbonimidic Diamide) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT3B/5-HT3A/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111332] [GtoPdb: 374, 373] [UniProtKB: O95264, P46098] | ||||||||
| ChEMBL | Agonist activity at human 5-HT43AB receptor expressed in Xenopus laevis oocytes | B | 5.55 | pEC50 | 2800 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 3207-3218 [PMID:28606760] |
| 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
| ChEMBL | Agonist activity at human 5-HT43A receptor expressed in Xenopus laevis oocytes | B | 5.42 | pEC50 | 3800 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 3207-3218 [PMID:28606760] |
| 5-HT3A/Serotonin 3a (5-HT3a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4972] [GtoPdb: 373] [UniProtKB: P23979] | ||||||||
| ChEMBL | Selectivity ratio of EC50 for mouse 5HT3A I187A receptor mutant to EC50 for wild type mouse 5HT3A receptor | B | 4.18 | pEC50 | 66000 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Agonist activity at mouse 5HT3A I187A receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method | F | 4.28 | pEC50 | 52000 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Selectivity ratio of EC50 for mouse 5HT3A S182A receptor mutant to EC50 for wild type mouse 5HT3A receptor | B | 4.47 | pEC50 | 34000 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Agonist activity at mouse 5HT3A S182A receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method | F | 4.57 | pEC50 | 27000 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Selectivity ratio of EC50 for mouse 5HT3A W183F receptor mutant to EC50 for wild type mouse 5HT3A receptor | B | 4.7 | pEC50 | 20000 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Agonist activity at mouse 5HT3A W183F receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method | F | 4.8 | pEC50 | 16000 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Selectivity ratio of EC50 for mouse 5HT3A Y153A receptor mutant to EC50 for wild type mouse 5HT3A receptor | B | 5.02 | pEC50 | 9600 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Agonist activity at mouse 5HT3A Y153A receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method | F | 5.12 | pEC50 | 7600 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Selectivity ratio of EC50 for mouse 5HT3A H185Y receptor mutant to EC50 for wild type mouse 5HT3A receptor | B | 5.17 | pEC50 | 6800 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Selectivity ratio of EC50 for mouse 5HT3A Y143F receptor mutant to EC50 for wild type mouse 5HT3A receptor | B | 5.17 | pEC50 | 6700 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Selectivity ratio of EC50 for mouse 5HT3A L184V receptor mutant to EC50 for wild type mouse 5HT3A receptor | B | 5.19 | pEC50 | 6400 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Agonist activity at mouse 5HT3A H185Y receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method | F | 5.27 | pEC50 | 5400 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Agonist activity at mouse 5HT3A Y143F receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method | F | 5.28 | pEC50 | 5300 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Agonist activity at mouse 5HT3A L184V receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method | F | 5.29 | pEC50 | 5100 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Selectivity ratio of EC50 for mouse 5HT3A H185F receptor mutant to EC50 for wild type mouse 5HT3A receptor | B | 5.49 | pEC50 | 3200 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Selectivity ratio of EC50 for mouse 5HT3A Q188A receptor mutant to EC50 for wild type mouse 5HT3A receptor | B | 5.54 | pEC50 | 2900 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Selectivity ratio of EC50 for mouse 5HT3A Y153F receptor mutant to EC50 for wild type mouse 5HT3A receptor | B | 5.55 | pEC50 | 2800 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Selectivity ratio of EC50 for mouse 5HT3A T181A receptor mutant to EC50 for wild type mouse 5HT3A receptor | B | 5.55 | pEC50 | 2800 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Agonist activity at mouse 5HT3A H185F receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method | F | 5.6 | pEC50 | 2500 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Selectivity ratio of EC50 for mouse 5HT3A I190V receptor mutant to EC50 for wild type mouse 5HT3A receptor | B | 5.6 | pEC50 | 2500 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Agonist activity at mouse 5HT3A Q188A receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method | F | 5.64 | pEC50 | 2300 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Agonist activity at mouse 5HT3A Y153F receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method | F | 5.66 | pEC50 | 2200 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Agonist activity at mouse 5HT3A T181A receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method | F | 5.66 | pEC50 | 2200 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Selectivity ratio of EC50 for mouse 5HT3A T186A receptor mutant to EC50 for wild type mouse 5HT3A receptor | B | 5.66 | pEC50 | 2200 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Agonist activity at mouse 5HT3A I190V receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method | F | 5.7 | pEC50 | 2000 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Agonist activity at mouse 5HT3A T186A receptor mutant expressed in Xenopus oocyte by two-electrode voltage patch method | F | 5.77 | pEC50 | 1700 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| ChEMBL | Agonist activity at wild type mouse 5HT3A receptor expressed in Xenopus oocyte by two-electrode voltage patch clamp method | F | 6.1 | pEC50 | 800 | nM | EC50 | Bioorg Med Chem (2009) 17: 5796-5805 [PMID:19640719] |
| 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-HT3A in Mouse [GtoPdb: 379] | ||||||||
| GtoPdb | - | - | 9 | pKd | - | - | - | Br J Pharmacol (1998) 123: 661-6 [PMID:9517385] |
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]
