CMPD-1 [Ligand Id: 1179] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL494803 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GnRH1 receptor/Gonadotropin-releasing hormone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1855] [GtoPdb: 256] [UniProtKB: P30968] | ||||||||
| ChEMBL | Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay | F | 7.72 | pKi | 19 | nM | Ki | Medchemcomm (2017) 8: 1965-1969 [PMID:30108717] |
| GtoPdb | - | - | 8.2 | pKi | - | - | - | J Pharmacol Exp Ther (2003) 305: 688-95 [PMID:12606616] |
| ChEMBL | Binding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assay | B | 8.22 | pKi | 6 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 1846-1850 [PMID:24613701] |
| ChEMBL | Displacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method | B | 8.22 | pKi | 6 | nM | Ki | Medchemcomm (2017) 8: 1965-1969 [PMID:30108717] |
| ChEMBL | Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay | F | 6 | pIC50 | 1000 | nM | IC50 | Medchemcomm (2017) 8: 1965-1969 [PMID:30108717] |
| GtoPdb | - | - | 7.8 | pIC50 | - | - | - | Biochemistry (2006) 45: 15327-37 [PMID:17176055] |
| GnRH1 receptor/Gonadotropin-releasing hormone receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3232679] [GtoPdb: 256] [UniProtKB: Q01776] | ||||||||
| ChEMBL | Binding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assay | B | 8.66 | pKi | 2.2 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 1846-1850 [PMID:24613701] |
| GnRH1 receptor/Gonadotropin-releasing hormone receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3066] [GtoPdb: 256] [UniProtKB: P30969] | ||||||||
| ChEMBL | Binding affinity at rat GnRH receptor by competition binding assay | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (2008) 51: 3331-3348 [PMID:18419112] |
| ChEMBL | Binding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assay | B | 8.42 | pKi | 3.8 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 1846-1850 [PMID:24613701] |
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]
