vidofludimus [Ligand Id: 9860] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL197194 (4SC-101, Imu-838, IMU-838, NSC-717824, SC-12267, SC12267, Vidofludimus) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Beta-lactamase NDM-1 in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295540] [UniProtKB: E5KIY2] | ||||||||
| ChEMBL | Binding affinity to Escherichia coli NDM-1 assessed as equilibrium dissociation constant measured for 60 sec by bio-layer interferometry analysis | B | 6.47 | pKd | 337 | nM | Kd | Eur J Med Chem (2023) 250: 115225-115225 [PMID:36870273] |
| ChEMBL | Inhibition of Escherichia coli NDM-1 expressed in Escherichia coli BL21 (DE3) using nitrocefin as substrate by microplate reader analysis | B | 4.86 | pIC50 | 13800 | nM | IC50 | Eur J Med Chem (2023) 250: 115225-115225 [PMID:36870273] |
| Bifunctional peptidase and (3S)-lysyl hydroxylase JMJD7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879430] [UniProtKB: P0C870] | ||||||||
| ChEMBL | Inhibition of N-terminal His-tagged human JMJD7 (1 to 316 residues) expressed in Escherichia coli BL21 (DE3) luciferase based succinate-gloTM JmjC demethylase/hydroxylase assay | B | 5.15 | pIC50 | 7160 | nM | IC50 | Bioorg Med Chem Lett (2021) 45: 128139-128139 [PMID:34048880] |
| Farnesoid X receptor/Bile acid receptor FXR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1] | ||||||||
| ChEMBL | Agonist activity at human FXR-LBD transfected in HEK293T cells co-transfected with pFR-Luc/pRL-SV40 assessed as transfection efficiency by measuring luciferase activity measured after 16 hrs by Gal4 hybrid reporter gene assay | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2023) 66: 6391-6402 [PMID:37127285] |
| ChEMBL | Agonist activity at FXR (unknown origin) | B | 6.35 | pEC50 | 450 | nM | EC50 | J Med Chem (2021) 64: 17545-17571 [PMID:34889100] |
| dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1966] [GtoPdb: 2604] [UniProtKB: Q02127] | ||||||||
| ChEMBL | Inhibition of human recombinant DHODH by colorimetric assay | B | 6.21 | pIC50 | 610 | nM | IC50 | J Med Chem (2023) 66: 6391-6402 [PMID:37127285] |
| ChEMBL | Inhibition of N-terminally truncated recombinant human dihydroorotate dehydrogenase using in vitro enzyme assay | B | 6.87 | pIC50 | 134 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4854-4857 [PMID:16143532] |
| ChEMBL | Inhibitory activity against recombinant human DHODH | B | 6.87 | pIC50 | 134 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 267-270 [PMID:16246558] |
| ChEMBL | Inhibition of human DHODH using dihydroorotate substrate by DCIP dye based spectrophotometry analysis | B | 6.87 | pIC50 | 134 | nM | IC50 | Eur J Med Chem (2022) 232: 114176-114176 [PMID:35151222] |
| GtoPdb | Determined in an indirect in vitro enzyme assay which measures the reduced co-substrate ubiquinone. | - | 7.32 | pIC50 | 48 | nM | IC50 | Am J Pathol (2010) 176: 2840-7 [PMID:20413687] |
| ChEMBL | Inhibition of DHODH in human HEK-293 cells transfected with ISRE-luciferase reporter gene assessed as increase in IFN-alpha mediated cellular response upto 72 hrs by luciferase reporter gene assay | B | 5.55 | pEC50 | 2800 | nM | EC50 | Eur J Med Chem (2020) 186: 111855-111855 [PMID:31740051] |
| ChEMBL | Inhibition of DHODH in human HEK-293 cells transfected with ISRE-luciferase reporter gene assessed as increase in IFN-alpha mediated cellular response upto 72 hrs by luciferase reporter gene assay | B | 5.56 | pEC50 | 2754.23 | nM | EC50 | Eur J Med Chem (2020) 186: 111855-111855 [PMID:31740051] |
| dihydroorotate dehydrogenase (quinone) in Mouse [GtoPdb: 2604] [UniProtKB: O35435] | ||||||||
| GtoPdb | - | - | 5.42 | pIC50 | 3800 | nM | IC50 | Am J Pathol (2010) 176: 2840-7 [PMID:20413687] |
| dihydroorotate dehydrogenase (quinone) in Rat [GtoPdb: 2604] [UniProtKB: Q63707] | ||||||||
| GtoPdb | - | - | 6.34 | pIC50 | 460 | nM | IC50 | Am J Pathol (2010) 176: 2840-7 [PMID:20413687] |
| Nerve Growth factor IB/Nuclear receptor subfamily 4 group A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293229] [GtoPdb: 629] [UniProtKB: P22736] | ||||||||
| ChEMBL | Agonist activity at Nur77 (unknown origin) by Gal4 hybrid reporter gene assay | B | 5.51 | pEC50 | 3100 | nM | EC50 | J Med Chem (2023) 66: 6391-6402 [PMID:37127285] |
| Nuclear receptor related 1/Nuclear receptor subfamily 4 group A member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5002] [GtoPdb: 630] [UniProtKB: P43354] | ||||||||
| ChEMBL | Binding affinity to recombinant N-terminal His6-tagged human Nurr1 LBD (362 to 598 residues) expressed in Escherichia coli BL21(DE3)-R3-pRARE2 by ITC method | B | 6.15 | pKd | 700 | nM | Kd | J Med Chem (2023) 66: 8170-8177 [PMID:37256819] |
| ChEMBL | Binding affinity to Nurr1-LBD (unknown origin) by Isothermal titration colorimetry | B | 6.15 | pKd | 700 | nM | Kd | J Med Chem (2023) 66: 6391-6402 [PMID:37127285] |
| ChEMBL | Agonist activity at human Nurr1 transfected in HEK293T cells co-transfected with pFR-Luc/pRL-SV40/pFA-CMV-hNurr1-LBD assessed as luciferase activity incubated for 16 hrs by Gal4 hybrid reporter gene based dual-glo luciferase assay | B | 6.4 | pEC50 | 400 | nM | EC50 | J Med Chem (2023) 66: 8170-8177 [PMID:37256819] |
| ChEMBL | Agonist activity at human Nurr1-LBD transfected in HEK293T cells co-transfected with pFR-Luc/pRL-SV40 assessed as transfection efficiency by measuring luciferase activity measured after 16 hrs by Gal4 hybrid reporter gene assay | B | 6.4 | pEC50 | 400 | nM | EC50 | J Med Chem (2023) 66: 6391-6402 [PMID:37127285] |
| GtoPdb | Determined in a Gal4-Nrr1 reporter gene assay | - | 6.4 | pEC50 | 400 | nM | EC50 | J Med Chem (2023) : |
| ChEMBL | Agonist activity at full length human Nurr1 transfected in HEK293T cells co-transfected with pFR-Luc-NRBE assessed as luciferase activity incubated for 16 hrs by dual-glo luciferase assay | B | 6.52 | pEC50 | 300 | nM | EC50 | J Med Chem (2023) 66: 8170-8177 [PMID:37256819] |
| Neuron-derived orphan receptor 1/Nuclear receptor subfamily 4 group A member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1961792] [GtoPdb: 631] [UniProtKB: Q92570] | ||||||||
| ChEMBL | Agonist activity at NOR1 (unknown origin) by Gal4 hybrid reporter gene assay | B | 5.54 | pEC50 | 2900 | nM | EC50 | J Med Chem (2023) 66: 6391-6402 [PMID:37127285] |
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869] | ||||||||
| ChEMBL | Agonist activity at human PPARalpha-LBD transfected in HEK293T cells co-transfected with pFR-Luc/pRL-SV40 assessed as transfection efficiency by measuring luciferase activity measured after 16 hrs by Gal4 hybrid reporter gene assay | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2023) 66: 6391-6402 [PMID:37127285] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| ChEMBL | Agonist activity at human PPARgamma-LBD transfected in HEK293T cells co-transfected with pFR-Luc/pRL-SV40 assessed as transfection efficiency by measuring luciferase activity measured after 16 hrs by Gal4 hybrid reporter gene assay | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2023) 66: 6391-6402 [PMID:37127285] |
| Retinoic acid receptor-α/Retinoic acid receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276] | ||||||||
| ChEMBL | Agonist activity at human RARalpha-LBD transfected in HEK293T cells co-transfected with pFR-Luc/pRL-SV40 assessed as transfection efficiency by measuring luciferase activity measured after 16 hrs by Gal4 hybrid reporter gene assay | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2023) 66: 6391-6402 [PMID:37127285] |
| Retinoid X receptor-α/Retinoid X receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793] | ||||||||
| ChEMBL | Agonist activity at human RXRalpha-LBD transfected in HEK293T cells co-transfected with pFR-Luc/pRL-SV40 assessed as transfection efficiency by measuring luciferase activity measured after 16 hrs by Gal4 hybrid reporter gene assay | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2023) 66: 6391-6402 [PMID:37127285] |
| Thyroid hormone receptor-α/Thyroid hormone receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1860] [GtoPdb: 588] [UniProtKB: P10827] | ||||||||
| ChEMBL | Agonist activity at human THRalpha-LBD transfected in HEK293T cells co-transfected with pFR-Luc/pRL-SV40 assessed as transfection efficiency by measuring luciferase activity measured after 16 hrs by Gal4 hybrid reporter gene assay | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2023) 66: 6391-6402 [PMID:37127285] |
| Vitamin D receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1977] [GtoPdb: 605] [UniProtKB: P11473] | ||||||||
| ChEMBL | Agonist activity at human VDR-LBD transfected in HEK293T cells co-transfected with pFR-Luc/pRL-SV40 assessed as transfection efficiency by measuring luciferase activity measured after 16 hrs by Gal4 hybrid reporter gene assay | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2023) 66: 6391-6402 [PMID:37127285] |
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]
