meta-chlorphenylbiguanide [Ligand Id: 2287] 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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  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Mouse [ChEMBL: CHEMBL4972] [GtoPdb: 373] [UniProtKB: P23979]
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  • 5-HT3AB in Human [GtoPdb: 378]
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  • 5-HT3A in Human [GtoPdb: 379]
  • 5-HT3A in Rat [GtoPdb: 379]
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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: 374373] [UniProtKB: O95264P46098]
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-HT3AB in Human [GtoPdb: 378]
GtoPdb - - 7 pKi - - - Neuropharmacology (2001) 41: 282-4 [PMID:11489465]
GtoPdb - - 5.7 pEC50 - - - Nature (1999) 397: 359-63 [PMID:9950429]
5-HT3A in Human [GtoPdb: 379]
GtoPdb - - 7.2 pKi - - - Mol Pharmacol (1995) 48: 407-16 [PMID:7565620];
Mol Pharmacol (1998) 53: 202-12 [PMID:9463477];
Neuropharmacology (2001) 41: 282-4 [PMID:11489465];
Br J Pharmacol (1996) 118: 1237-45 [PMID:8818349];
Eur J Pharmacol (2000) 409: 195-201 [PMID:11104834]
GtoPdb - - 5.8 pEC50 1600 nM EC50 Nature (1999) 397: 359-63 [PMID:9950429];
Mol Pharmacol (1995) 48: 1054-62 [PMID:8848005];
Mol Pharmacol (1995) 48: 407-16 [PMID:7565620];
Mol Pharmacol (1998) 53: 202-12 [PMID:9463477];
Eur J Pharmacol (1999) 369: 125-32 [PMID:10204690]
5-HT3A in Rat [GtoPdb: 379]
GtoPdb - - 9 pKi - - - Mol Pharmacol (1995) 48: 407-16 [PMID:7565620];
Br J Pharmacol (1998) 123: 661-6 [PMID:9517385]
GtoPdb - - 6.9 pEC50 - - - Br J Pharmacol (1998) 124: 1667-74 [PMID:9756382];
Eur J Pharmacol (1999) 369: 125-32 [PMID:10204690]

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]