MK-7725 [Ligand Id: 8502] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2023109 (MK-7725) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| BB3 receptor/Bombesin receptor subtype-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4080] [GtoPdb: 40] [UniProtKB: P32247] | ||||||||
| ChEMBL | Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting | B | 8.44 | pIC50 | 3.6 | nM | IC50 | Bioorg Med Chem (2012) 20: 2845-2849 [PMID:22494842] |
| ChEMBL | Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting | B | 8.44 | pIC50 | 3.6 | nM | IC50 | ACS Med Chem Lett (2012) 3: 252-256 [PMID:24900461] |
| GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 | ACS Med Chem Lett (2012) 3: 252-6 [PMID:24900461] |
| ChEMBL | Agonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay | F | 7.14 | pEC50 | 73 | nM | EC50 | Bioorg Med Chem (2012) 20: 2845-2849 [PMID:22494842] |
| ChEMBL | Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay | B | 7.14 | pEC50 | 73 | nM | EC50 | Bioorg Med Chem (2015) 23: 89-104 [PMID:25497965] |
| ChEMBL | Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay | B | 8.85 | pEC50 | 1.4 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 750-755 [PMID:24412111] |
| BB3 receptor/Bombesin receptor subtype-3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075140] [GtoPdb: 40] [UniProtKB: O54798] | ||||||||
| ChEMBL | Agonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay | F | 6.89 | pEC50 | 130 | nM | EC50 | Bioorg Med Chem (2012) 20: 2845-2849 [PMID:22494842] |
| ChEMBL | Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay | F | 6.89 | pEC50 | 130 | nM | EC50 | ACS Med Chem Lett (2012) 3: 252-256 [PMID:24900461] |
| ChEMBL | Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay | B | 6.89 | pEC50 | 130 | nM | EC50 | Bioorg Med Chem (2015) 23: 89-104 [PMID:25497965] |
| ChEMBL | Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay | B | 7.66 | pEC50 | 22 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 750-755 [PMID:24412111] |
| Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469] | ||||||||
| ChEMBL | Activation of PXR | B | 4.52 | pEC50 | >30000 | nM | EC50 | ACS Med Chem Lett (2012) 3: 252-256 [PMID:24900461] |
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]
