PSB-1584 [Ligand Id: 10717] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL124977
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GPR84/G-protein coupled receptor 84 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3714079] [GtoPdb: 120] [UniProtKB: Q9NQS5]
ChEMBL Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method B 8.53 pKi 2.98 nM Ki J Med Chem (2020) 63: 2391-2410 [PMID:31721581]
GtoPdb Potency in a cAMP assay. - 8.3 pEC50 5 nM EC50 ACS Omega (2018) 3: 3365-3383 [PMID:30023867]
ChEMBL Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assay F 8.31 pEC50 4.93 nM EC50 J Med Chem (2020) 63: 2391-2410 [PMID:31721581]
GtoPdb Potency in a β-arrestin recruitment assay. - 8.49 pEC50 3.2 nM EC50 ACS Omega (2018) 3: 3365-3383 [PMID:30023867]
ChEMBL Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay B 8.5 pEC50 3.18 nM EC50 J Med Chem (2020) 63: 2391-2410 [PMID:31721581]

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]