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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]