example 184 [WO2014186035] [Ligand Id: 12668] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4279060 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| indoleamine 2,3-dioxygenase 1/Indoleamine 2,3-dioxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4685] [GtoPdb: 2829] [UniProtKB: P14902] | ||||||||
| ChEMBL | Inhibition of recombinant human N-terminal His-tagged IDO1 (1 to 403 residues) expressed in Escherichia coli assessed as reduction in kynurenine formation using tryptophan as substrate measured by LC/MS/MS analysis | B | 6.7 | pIC50 | <200 | nM | IC50 | US-20160046596-A1. Inhibitors of the kynurenine pathway (2016) |
| ChEMBL | Inhibition of IDO1 in IFNgamma-stimulated human HeLa cells assessed as reduction in kynurenine formation using L-tryptophan as substrate measured after 15 mins by UV-vis HPLC analysis | B | 6.7 | pIC50 | <200 | nM | IC50 | US-20160046596-A1. Inhibitors of the kynurenine pathway (2016) |
| indoleamine 2,3-dioxygenase 2/Indoleamine 2,3-dioxygenase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3627587] [GtoPdb: 3019] [UniProtKB: Q6ZQW0] | ||||||||
| GtoPdb | Inhibition of recombinant human IDO2 (14-420)-mediated kynurenine formation from tryptophan, detected by LC/MS/MS analysis | - | 6 | pIC50 | <1000 | nM | IC50 | WO2014186035A1. Inhibitors of the kynurenine pathway (2014) |
| ChEMBL | Inhibition of recombinant human C-terminal polyHis-tagged IDO2 (Met14 to Gly420 residues) expressed in Escherichia coli assessed as reduction in kynurenine formation using tryptophan as substrate measured by LC/MS/MS analysis | B | 6 | pIC50 | <1000 | nM | IC50 | US-20160046596-A1. Inhibitors of the kynurenine pathway (2016) |
| tryptophan 2,3-dioxygenase/Tryptophan 2,3-dioxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2140] [GtoPdb: 2887] [UniProtKB: P48775] | ||||||||
| ChEMBL | Inhibition of recombinant human TDO2 expressed in CHOK1 cells assessed as reduction in kynurenine formation using L-tryptophan as substrate measured after 2 hrs by LC/MS/MS analysis | B | 6.3 | pIC50 | <500 | nM | IC50 | US-20160046596-A1. Inhibitors of the kynurenine pathway (2016) |
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]
