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 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]
