[3H]GR65630 [Ligand Id: 2303] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL122903 (GR-65630)
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 3 (5-HT3) receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 Rat024681012Highcharts.com
  • 5-HT3A in Human [GtoPdb: 379]
Created with Highcharts 10.3.3ValuesChart context menu5-HT3ApKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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: 377374373376375] [UniProtKB: A5X5Y0O95264P46098Q70Z44Q8WXA8]
ChEMBL Potency to 5-hydroxytryptamine 3 receptor using [3H]GR-65630 as radioligand in rat cortex B 8.79 pKi 1.62 nM Ki J Med Chem (1990) 33: 1594-1600 [PMID:2342053]
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373374] [UniProtKB: P35563Q9JJ16]
ChEMBL Displacement of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor in rat brain cortical membranes B 9.55 pKi 0.28 nM Ki J Med Chem (1993) 36: 3693-3699 [PMID:8246239]
5-HT3A in Human [GtoPdb: 379]
GtoPdb - - 9.32 pKd 0.48 nM Kd Mol Pharmacol (1998) 53: 202-12 [PMID:9463477];
J Pharmacol Sci (2007) 104: 263-73 [PMID:17652911]

ChEMBL data shown on this page come from version 35:

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]