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 |
|---|---|---|---|---|---|---|---|---|
| FPR1/Formyl peptide receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3359] [GtoPdb: 222] [UniProtKB: P21462] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: FPR1 | F | 5.22 | pIC50 | 6029.7 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| GPR119/Glucose-dependent insulinotropic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5652] [GtoPdb: 126] [UniProtKB: Q8TDV5] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR119 | F | 5.35 | pIC50 | 4423.95 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| 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] |
| GPR183/G-protein coupled receptor 183 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3259470] [GtoPdb: 81] [UniProtKB: P32249] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183 | F | 5.43 | pIC50 | 3754.81 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| FPR3/N-formyl peptide receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5646] [GtoPdb: 224] [UniProtKB: P25089] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: FPR3 | F | 5 | pIC50 | >10000 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
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]
