PD 165929 [Ligand Id: 620] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL86828 (PD-165929)
  • 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]
  • BB1 receptor/Neuromedin B receptor in Rat [ChEMBL: CHEMBL4440] [GtoPdb: 38] [UniProtKB: P24053]
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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]
ChEMBL In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin. B 5 pKi >10000 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 5 pKi >10000 nM Ki Bioorg Med Chem Lett (1996) 6: 2617-2622
BB1 receptor/Neuromedin B receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3636] [GtoPdb: 38] [UniProtKB: P28336]
GtoPdb - - 8.2 pKd 6.31 nM Kd Bioorg Med Chem Lett (1996) 6: 2617-2622
ChEMBL Antagonism of recombinant human bombesin receptor (bb1) labeled with [125I]- [Tyr] bombesin stably expressed in CHO cells F 8.2 pKi 6.3 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 8.2 pKi 6.3 nM Ki Bioorg Med Chem Lett (1996) 6: 2617-2622
ChEMBL Binding affinity against human NMB receptor was determined B 8.2 pKi 6.3 nM Ki Bioorg Med Chem Lett (1996) 6: 2617-2622
ChEMBL Affinity of [125I][D-Tyr0]-NMB to human Neuromedin B receptor expressed in HEK293 cells B 6.46 pIC50 350 nM IC50 Bioorg Med Chem Lett (2004) 14: 3037-3042 [PMID:15149640]
BB1 receptor/Neuromedin B receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4440] [GtoPdb: 38] [UniProtKB: P24053]
ChEMBL Binding affinity against NMB receptor in rat olfactory bulb was determined using [125I]-[Tyr4] bombesin. B 6.82 pIC50 150 nM IC50 Bioorg Med Chem Lett (1996) 6: 2617-2622

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]