bag-1 [Ligand Id: 6188] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL1091720
  • BB3 receptor/Bombesin receptor subtype-3 in Human [ChEMBL: CHEMBL4080] [GtoPdb: 40] [UniProtKB: P32247]
  • BB3 receptor/Bombesin receptor subtype-3 in Mouse [ChEMBL: CHEMBL1075140] [GtoPdb: 40] [UniProtKB: O54798]
  • BB3 receptor/Bombesin receptor subtype-3 in Rat [ChEMBL: CHEMBL1075111] [GtoPdb: 40] [UniProtKB: Q8K418]
There should be some charts here, you may need to enable JavaScript!
  • BB2 receptor/Gastrin releasing peptide receptor in Human [ChEMBL: CHEMBL4959] [GtoPdb: 39] [UniProtKB: P30550]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • BB1 receptor/Neuromedin B receptor in Human [ChEMBL: CHEMBL3636] [GtoPdb: 38] [UniProtKB: P28336]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
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 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]