compound 8a [PMID: 24900283] [Ligand Id: 8503] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2164575 |
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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]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting | B | 6.77 | pIC50 | 169 | nM | IC50 | ACS Med Chem Lett (2011) 2: 933-937 [PMID:24900283] |
| GtoPdb | - | - | 8.85 | pIC50 | 1.4 | nM | IC50 | ACS Med Chem Lett (2011) 2: 933-7 [PMID:24900283] |
| ChEMBL | Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting | B | 8.85 | pIC50 | 1.4 | nM | IC50 | ACS Med Chem Lett (2011) 2: 933-937 [PMID:24900283] |
| ChEMBL | Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay | F | 5 | pEC50 | >10000 | nM | EC50 | ACS Med Chem Lett (2011) 2: 933-937 [PMID:24900283] |
| ChEMBL | Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay | F | 7.01 | pEC50 | 97 | nM | EC50 | ACS Med Chem Lett (2011) 2: 933-937 [PMID:24900283] |
| ChEMBL | Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay | B | 7.01 | pEC50 | 97 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 750-755 [PMID:24412111] |
| ChEMBL | Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay | B | 7.01 | pEC50 | 97 | nM | EC50 | Bioorg Med Chem (2015) 23: 89-104 [PMID:25497965] |
| ChEMBL | Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 10 mins by bioluminescence assay | F | 7.82 | pEC50 | 15 | nM | EC50 | ACS Med Chem Lett (2011) 2: 933-937 [PMID:24900283] |
| 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 HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay | F | 5 | pEC50 | >10000 | nM | EC50 | ACS Med Chem Lett (2011) 2: 933-937 [PMID:24900283] |
| ChEMBL | Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay | F | 7.48 | pEC50 | 33 | nM | EC50 | ACS Med Chem Lett (2011) 2: 933-937 [PMID:24900283] |
| ChEMBL | Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay | B | 7.48 | pEC50 | 33 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 750-755 [PMID:24412111] |
| ChEMBL | Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay | B | 7.48 | pEC50 | 33 | nM | EC50 | Bioorg Med Chem (2015) 23: 89-104 [PMID:25497965] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2011) 2: 933-937 [PMID:24900283] |
| Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469] | ||||||||
| ChEMBL | Activation of human PXR | B | 6.17 | pEC50 | 678 | nM | EC50 | ACS Med Chem Lett (2011) 2: 933-937 [PMID:24900283] |
| ChEMBL | Activation of PXR | B | 6.17 | pEC50 | 677 | 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]
