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, 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 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]