NIBR189 [Ligand Id: 13052] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3262896
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GPR183/G-protein coupled receptor 183 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3259470] [GtoPdb: 81] [UniProtKB: P32249]
ChEMBL Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay F 7.96 pIC50 11 nM IC50 J Med Chem (2014) 57: 3358-3368 [PMID:24678947]
GtoPdb Antagonism of NIBR51-induced GPR183 activation - 7.96 pIC50 11 nM IC50 J Med Chem (2014) 57: 3358-68 [PMID:24678947]
ChEMBL Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay F 7.98 pIC50 10.47 nM IC50 J Med Chem (2014) 57: 3358-3368 [PMID:24678947]
ChEMBL Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assay F 8.05 pIC50 9 nM IC50 J Med Chem (2014) 57: 3358-3368 [PMID:24678947]
ChEMBL Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assay F 8.06 pIC50 8.71 nM IC50 J Med Chem (2014) 57: 3358-3368 [PMID:24678947]
ChEMBL Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis F 8.07 pIC50 8.51 nM IC50 J Med Chem (2014) 57: 3358-3368 [PMID:24678947]
ChEMBL Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis F 8.07 pIC50 8.5 nM IC50 J Med Chem (2014) 57: 3358-3368 [PMID:24678947]
ChEMBL Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis F 8.15 pIC50 7.08 nM IC50 J Med Chem (2014) 57: 3358-3368 [PMID:24678947]
ChEMBL Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis F 8.15 pIC50 7 nM IC50 J Med Chem (2014) 57: 3358-3368 [PMID:24678947]
ChEMBL Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysis B 9.52 pIC50 0.3 nM IC50 J Med Chem (2014) 57: 3358-3368 [PMID:24678947]
ChEMBL Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysis B 9.65 pIC50 0.22 nM IC50 J Med Chem (2014) 57: 3358-3368 [PMID:24678947]
GPR183/G-protein coupled receptor 183 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3259471] [GtoPdb: 81] [UniProtKB: Q3U6B2]
GtoPdb Antagonism of NIBR51-induced GPR183 activation - 7.82 pIC50 15 nM IC50 J Med Chem (2014) 57: 3358-68 [PMID:24678947]
ChEMBL Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay F 7.82 pIC50 15 nM IC50 J Med Chem (2014) 57: 3358-3368 [PMID:24678947]
ChEMBL Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay F 7.86 pIC50 13.8 nM IC50 J Med Chem (2014) 57: 3358-3368 [PMID:24678947]

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]