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 human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay | F | 7.41 | pIC50 | 38.6 | nM | IC50 | J Med Chem (2023) 66: 15926-15943 [PMID:38047891] |
| 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 | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183 | F | 8.97 | pIC50 | 1.08 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| 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 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]
