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 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]
