examorelin [Ligand Id: 1100] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL108335 (EP-23905, Examorelin, Hexarelin, MF-6003)
  • ghrelin receptor/Ghrelin receptor in Human [ChEMBL: CHEMBL4616] [GtoPdb: 246] [UniProtKB: Q92847]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ghrelin receptor/Ghrelin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4616] [GtoPdb: 246] [UniProtKB: Q92847]
GtoPdb - - 7.89 pKd 13 nM Kd J Clin Endocrinol Metab (2000) 85: 3803-7 [PMID:11061542]
ChEMBL Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand B 7.74 pIC50 18 nM IC50 J Med Chem (2003) 46: 1191-1203 [PMID:12646029]
ChEMBL Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method B 7.8 pIC50 15.9 nM IC50 J Med Chem (2012) 55: 6502-6511 [PMID:22712585]
Platelet glycoprotein 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163174] [UniProtKB: Q07969]
ChEMBL Displacement of photoactivatable [125I]-Tyr-Bpa-Ala-hexarelin from CD36 in Sprague-Dawley rat cardiac membranes incubated for 60 mins and followed by UV irradiation and measured after 15 mins by radioligand binding assay B 5.53 pIC50 2970 nM IC50 US-20130203686-A1. Azapeptides as cd36 binding compounds (null)
ChEMBL Displacement of photoactivatable [125I]-Tyr-Bpa-Ala-Hexarelin from CD36 in Sprague-Dawley rat cardiac membranes incubated for 60 mins by densitometry B 5.68 pIC50 2080 nM IC50 J Med Chem (2012) 55: 6502-6511 [PMID:22712585]
ChEMBL Inhibition of photoactivatable [125I]-Tyr-Bpa-Ala-hexarelin binding to CD36 in Sprague-Dawley rat heart membranes after 60 mins by SDS-PAGE analysis B 5.81 pIC50 1560 nM IC50 J Med Chem (2017) 60: 9263-9274 [PMID:29028172]
ChEMBL Displacement of [125]-Tyr-Bpa-Ala-Hexarelin from CD36 in Sprague-Dawley rat heart membranes incubated for 60 mins B 6.3 pIC50 500 nM IC50 WO-2018000079-A1. Novel cyclic peptides and uses thereof (null)

ChEMBL data shown on this page come from version 33:

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]