maxacalcitol [Ligand Id: 2784] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL333950 (1alpha,25-dihydroxy-22-oxavitamin d3, 22-oxacalcitriol, Maxacalcitol, OCT, Oxarol, Prezios, SCH 209579, SCH-209579)
  • Vitamin D receptor in Human [ChEMBL: CHEMBL1977] [GtoPdb: 605] [UniProtKB: P11473]
  • Vitamin D receptor in Rat [GtoPdb: 605] [UniProtKB: P13053]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Vitamin D receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1977] [GtoPdb: 605] [UniProtKB: P11473]
ChEMBL Activation of VDR in human HaCaT cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay B 6.8 pEC50 159.7 nM EC50 J Med Chem (2016) 59: 5102-5108 [PMID:27070779]
ChEMBL Activation of VDR in human Caco2 cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay B 6.84 pEC50 144.5 nM EC50 J Med Chem (2016) 59: 5102-5108 [PMID:27070779]
ChEMBL Transactivation of VDR in human Caco2 cells after 24 hrs by luciferase reporter gene assay B 7.39 pEC50 40.8 nM EC50 J Med Chem (2015) 58: 7881-7887 [PMID:26367019]
ChEMBL Transactivation of VDR in human HaCaT cells after 24 hrs by luciferase reporter gene assay B 7.42 pEC50 37.9 nM EC50 J Med Chem (2015) 58: 7881-7887 [PMID:26367019]
ChEMBL Activation of VDR in human Jurkat cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay B 9.07 pEC50 0.85 nM EC50 J Med Chem (2016) 59: 5102-5108 [PMID:27070779]
Vitamin D receptor in Rat [GtoPdb: 605] [UniProtKB: P13053]
GtoPdb - - 8.21 pEC50 - - - Bone (1993) 14: 47-51 [PMID:8443002]

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]