bag-1 [Ligand Id: 6188] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1091720 |
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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] | ||||||||
| GtoPdb | - | - | 7.74 | pIC50 | 18.3 | nM | IC50 | Cell Metab (2010) 11: 101-12 [PMID:20096642] |
| ChEMBL | Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 2074-2077 [PMID:20219372] |
| ChEMBL | Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin | F | 7 | pEC50 | 99 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 2074-2077 [PMID:20219372] |
| ChEMBL | Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay | F | 7.33 | pEC50 | 47 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 2074-2077 [PMID:20219372] |
| ChEMBL | Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay | F | 7.33 | pEC50 | 47 | nM | EC50 | ACS Med Chem Lett (2011) 2: 43-47 [PMID:24900253] |
| BB3 receptor/Bombesin receptor subtype-3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075140] [GtoPdb: 40] [UniProtKB: O54798] | ||||||||
| GtoPdb | - | - | 8.16 | pIC50 | 6.9 | nM | IC50 | Cell Metab (2010) 11: 101-12 [PMID:20096642] |
| ChEMBL | Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from mouse BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting | B | 8.16 | pIC50 | 6.9 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 2074-2077 [PMID:20219372] |
| ChEMBL | Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin | F | 7.11 | pEC50 | 78 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 2074-2077 [PMID:20219372] |
| ChEMBL | Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay | F | 8.55 | pEC50 | 2.8 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 2074-2077 [PMID:20219372] |
| BB3 receptor/Bombesin receptor subtype-3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075111] [GtoPdb: 40] [UniProtKB: Q8K418] | ||||||||
| ChEMBL | Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from rat BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting | B | 8.62 | pIC50 | 2.4 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 2074-2077 [PMID:20219372] |
| GtoPdb | - | - | 8.62 | pIC50 | 2.4 | nM | IC50 | Cell Metab (2010) 11: 101-12 [PMID:20096642] |
| BB2 receptor/Gastrin releasing peptide receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4959] [GtoPdb: 39] [UniProtKB: P30550] | ||||||||
| ChEMBL | Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human GRP-R expressed in NFAT-CHO cells after 2 hrs by scintillation counting | B | 5.19 | pIC50 | 6400 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 2074-2077 [PMID:20219372] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 5.92 | pIC50 | 1200 | nM | IC50 | ACS Med Chem Lett (2011) 2: 43-47 [PMID:24900253] |
| BB1 receptor/Neuromedin B receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3636] [GtoPdb: 38] [UniProtKB: P28336] | ||||||||
| ChEMBL | Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human NMB-R expressed in NFAT-CHO cells after 2 hrs by scintillation counting | B | 5.15 | pIC50 | 7000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 2074-2077 [PMID:20219372] |
| Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469] | ||||||||
| ChEMBL | Activation of human PXR | B | 5.46 | pIC50 | 3500 | nM | IC50 | ACS Med Chem Lett (2011) 2: 43-47 [PMID:24900253] |
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]
