examorelin [Ligand Id: 1100] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL108335 (EP-23905, Examorelin, Examorelina, Examoreline, Hexarelin, MF-6003) |
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| 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 (2013) |
| 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 (2018) |
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]
