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 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]