bombesin [Ligand Id: 616] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL437027 (Bombesin)
  • BB2 receptor/Gastrin releasing peptide receptor in Human [ChEMBL: CHEMBL4959] [GtoPdb: 39] [UniProtKB: P30550]
  • BB2 receptor in Mouse [GtoPdb: 39] [UniProtKB: P21729]
  • BB2 receptor in Rat [GtoPdb: 39] [UniProtKB: P52500]
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  • BB1 receptor/Neuromedin B receptor in Human [ChEMBL: CHEMBL3636] [GtoPdb: 38] [UniProtKB: P28336]
  • BB1 receptor in Rat [GtoPdb: 38] [UniProtKB: P24053]
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  • Y1 receptor/Neuropeptide Y receptor type 1 in Human [ChEMBL: CHEMBL4777] [GtoPdb: 305] [UniProtKB: P25929]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
BB2 receptor/Gastrin releasing peptide receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4959] [GtoPdb: 39] [UniProtKB: P30550]
GtoPdb - - 8.85 pKi 1.4 nM Ki J Pharmacol Exp Ther (1999) 290: 1202-11 [PMID:10454496];
Mol Pharmacol (1995) 47: 10-20 [PMID:7838118]
ChEMBL In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin. B 9.82 pKi 0.15 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 2589-2594 [PMID:9873586]
ChEMBL Binding affinity against [125 I][4Tyr]-bombesin labeled cloned human GRP(gastrin releasing peptide) receptors stably expressed in CHO cells B 9.82 pKi 0.15 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 2617-2622
ChEMBL Displacement of [125I]-Tyr4-BBN from human GRPR overexpressed in human T47D cells B 8.7 pIC50 2 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 687-692 [PMID:23265893]
GtoPdb - - 10.15 pIC50 0.07 nM IC50 Peptides (2011) 32: 1685-99 [PMID:21729729]
ChEMBL Displacement of 125I[Tyr4]-bombesin from GRPR expressed in human PC3 cells B 9.59 pEC50 0.26 nM EC50 Bioorg. Med. Chem. Lett. (2008) 18: 2424-2427 [PMID:18329268]
BB2 receptor in Mouse [GtoPdb: 39] [UniProtKB: P21729]
GtoPdb - - 9.05 pKi 0.9 nM Ki Mol Pharmacol (1995) 47: 10-20 [PMID:7838118]
BB2 receptor in Rat [GtoPdb: 39] [UniProtKB: P52500]
GtoPdb - - 8.39 pKi 4.1 nM Ki Mol Pharmacol (1995) 47: 10-20 [PMID:7838118]
BB1 receptor/Neuromedin B receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3636] [GtoPdb: 38] [UniProtKB: P28336]
GtoPdb - - 7.49 pKi 32 nM Ki J Pharmacol Exp Ther (1999) 290: 1202-11 [PMID:10454496];
Mol Pharmacol (1995) 47: 10-20 [PMID:7838118]
ChEMBL Antagonism of recombinant human bombesin receptor (bb1) labeled with [125I]- [Tyr] bombesin stably expressed in CHO cells F 8.7 pKi 2 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 2589-2594 [PMID:9873586]
ChEMBL Binding affinity against [125 I][4Tyr]-bombesin labeled cloned human NMB receptor stably expressed in CHO cells B 8.7 pKi 2 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 2617-2622
GtoPdb - - 8.75 pIC50 1.77 nM IC50 Peptides (2011) 32: 1685-99 [PMID:21729729]
BB1 receptor in Rat [GtoPdb: 38] [UniProtKB: P24053]
GtoPdb - - 7.68 pKi 21 nM Ki J Pharmacol Exp Ther (1999) 290: 1202-11 [PMID:10454496];
Mol Pharmacol (1995) 47: 10-20 [PMID:7838118]
Y1 receptor/Neuropeptide Y receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4777] [GtoPdb: 305] [UniProtKB: P25929]
ChEMBL Displacement of [125I]-NPY from Y1 receptor in human MCF7 cells B 8.33 pIC50 4.7 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 687-692 [PMID:23265893]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]