PD 176252 [Ligand Id: 626] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL405908
  • BB2 receptor/Gastrin releasing peptide receptor in Human [ChEMBL: CHEMBL4959] [GtoPdb: 39] [UniProtKB: P30550]
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  • BB1 receptor/Neuromedin B receptor in Human [ChEMBL: CHEMBL3636] [GtoPdb: 38] [UniProtKB: P28336]
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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 - - 9 pKi 1 nM Ki Bioorg Med Chem Lett (1998) 8: 2589-94 [PMID:9873586]
ChEMBL Antagonistic activity against cloned human Bombesin receptor bb2 labeled with [125I]- [Tyr] bombesin stably expressed in CHO cells; 0.66-1.3 F 9 pKi 1 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 2589-2594 [PMID:9873586]
GtoPdb - - 6.77 pIC50 170 nM IC50 Peptides (2009) 30: 1473-86 [PMID:19463875]
GtoPdb - - 6.77 pIC50 170 nM IC50 Peptides (2009) 30: 1473-86 [PMID:19463875]
ChEMBL Antagonistic activity against labelled Bombesin receptor bb2 binding sites in rat cerebral cortex by using [125I]- [Tyr] bombesin in presence of NMB; 6.5-31 B 7.8 pIC50 16 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 2589-2594 [PMID:9873586]
BB1 receptor/Neuromedin B receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3636] [GtoPdb: 38] [UniProtKB: P28336]
ChEMBL Antagonism of recombinant human bombesin receptor (bb1) labeled with [125I]- [Tyr] bombesin stably expressed in CHO cells F 9.77 pKi 0.17 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 2589-2594 [PMID:9873586]
ChEMBL Antagonistic activity against labelled Bombesin receptor bb1 binding sites in rat olfactory bulb by using [125I]- [Tyr] bombesin in presence of [D-Phe-6] bombesin(6-13)ethyl ester; 0.31-1.3 B 9.18 pIC50 0.66 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 2589-2594 [PMID:9873586]
GtoPdb - - 9.77 pIC50 0.17 nM IC50 Peptides (2009) 30: 1473-86 [PMID:19463875]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]