Calcitriol (CID 5280453) - BioAssay Data Summary for Compound
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BioActivity Outcomes:
Active(125)
 
 
Top Targets:
NR LBD VDR(48)
 
 
LRR RI(3)
 
 
ALBUMIN(1)
 
 
Anoctamin(1)
 
 
CARD NOD1 CAR..(1)
 
 
BioAssay Types:
Literature(95)
 
 
Screening(11)
 
 
Confirmatory(4)
 
 
BioActivity Types:
EC50(29)
 
 
IC50(19)
 
 
Ki(11)
 
 
Kd(3)
 
 
Potency(3)
 
 
SAR
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Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 125    Data Row: 125   Total Pages: 3   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103221863]
EC50 1e-05Activity at human VDR expressed in human HOS cells transfected with pGL3-hOc, pCDNA-hVDR and phRL-TK assessed as assessed as transcriptional activation measured 24 hrs post infection by luciferase reporter gene assay [AID622098, Type: Literature]Vitamin D3 receptor [gi:137617]
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2
[SID103221863]
EC50 1e-05Activity at human VDR expressed in human HOS cells transfected with pGL3-hOc, pCDNA-hVDR and phRL-TK assessed as assessed as transcriptional activation measured 24 hrs post infection by luciferase reporter gene assay [AID622098, Type: Literature]Vitamin D3 receptor [gi:137617]
View
3
[SID103221863]
EC50 1e-05Activity at human VDR expressed in human HOS cells transfected with pGL3-hOc, pCDNA-hVDR and phRL-TK assessed as assessed as transcriptional activation measured 24 hrs post infection by luciferase reporter gene assay [AID622098, Type: Literature]Vitamin D3 receptor [gi:137617]
View
4
[SID103221863]
EC50 1e-05Activity at human VDR expressed in human HOS cells transfected with pGL3-hOc, pCDNA-hVDR and phRL-TK assessed as assessed as transcriptional activation measured 24 hrs post infection by luciferase reporter gene assay [AID622098, Type: Literature]Vitamin D3 receptor [gi:137617]
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5
[SID103221863]
EC50 1.06e-05Effect on VDR transcriptional activity in human osteosarcoma cells [AID321740, Type: Literature]Vitamin D3 receptor [gi:137617]
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6
[SID103221863]
EC50 1.06e-05Effect on VDR transcriptional activity in human osteosarcoma cells [AID321740, Type: Literature]Vitamin D3 receptor [gi:137617]
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7
[SID103221863]
EC50 1.06e-05Effect on VDR transcriptional activity in human osteosarcoma cells [AID321740, Type: Literature]Vitamin D3 receptor [gi:137617]
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8
[SID103221863]
EC50 1.06e-05Effect on VDR transcriptional activity in human osteosarcoma cells [AID321740, Type: Literature]Vitamin D3 receptor [gi:137617]
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9
[SID103221863]
Ki 2.5e-05Displacement from vitamin D receptor in chick intestine : 50% displacement [AID216827, Type: other]Vitamin D3 receptor [gi:3915243]
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10
[SID103221863]
IC50 2.9e-05Inhibition of LPS-induced TNFalpha production in human PBMC after 24 hrs by ELISA [AID414857, Type: Literature]
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11
[SID103221863]
IC50 3e-05Antiproliferative activity against mouse LM05e cells assessed as decrease in cell number after 72 hrs by WST assay [AID652552, Type: other]
View
12
[SID103221863]
IC50 5e-05Concentration to inhibit T-cell activation in Murine MLR [AID210294, Type: other]
View
13
[SID103221863]
Ki 5e-05Displacement of [3H]1-alpha,25-(OH)2D3 from rat recombinant full length VDR [AID387114, Type: Literature]Vitamin D3 receptor [gi:137618]
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14
[SID103221863]
EC50 5e-05Displacement of 1-alpha,25-dihydroxyvitamin from rat recombinant VDR [AID303407, Type: Literature]Vitamin D3 receptor [gi:137618]
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15
[SID103221863]
EC50 5e-05Displacement of [3H]1,25-(OH)2D3 from bovine thymus vitamin D receptor [AID366868, Type: Literature]Vitamin D3 receptor [gi:161784270]
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16
[SID103221863]
Kd 6.5e-05Binding affinity to VDR receptor [AID217167, Type: Literature]
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17
[SID103221863]
Kd 7e-05Displacement of [3H]1-alpha,25-(OH)2D3 from VDR in pig intestinal mucosa [AID472015, Type: Literature]Vitamin D3 receptor [gi:190411613]
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18
[SID103221863]
EC50 7.1e-05Displacement of [3H]1,25-(OH)2D3 from vitamin D receptor in bovine thymus [AID280114, Type: Literature]Vitamin D3 receptor [gi:161784270]
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19
[SID103221863]
Ki 0.0001Displacement of [3H]1alpha,25-(OH)2D3 from rat recombinant full length VDR [AID547392, Type: Literature]Vitamin D3 receptor [gi:137618]
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20
[SID103221863]
Ki 0.0001Displacement of radiolabeled 1alpha, 25-(OH)2D3 from recombinant rat VDR [AID619442, Type: Literature]Vitamin D3 receptor [gi:137618]
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21
[SID103221863]
EC50 0.0001Displacement of [3H]1,25-(OH)2D3 from rat recombinant His-tagged VDR ligand-binding domain expressed in Escherichia coli BL21 [AID326337, Type: Literature]Vitamin D3 receptor [gi:137618]
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22
[SID103221863]
Ki 0.0001Displacement of [3H]1-alpha,25-(OH)2D3 from rat recombinant full length VDR [AID351849, Type: Literature]Vitamin D3 receptor [gi:137618]
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23
[SID103221863]
Ki 0.0001Displacement of [3H]-1alpha,25(OH)2D3 from recombinant rat VDR by scintillation counting [AID635571, Type: Literature]Vitamin D3 receptor [gi:137618]
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24
[SID103221863]
Ki 0.0001Displacement of [3H]-1alpha,25(OH)2D3 from recombinant rat VDR after overnight incubation by scintillation counting [AID672798, Type: Literature]Vitamin D3 receptor [gi:137618]
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25
[SID103221863]
Ki 0.0001Displacement of [3H]1-alpha,25-(OH)2D3 from rat recombinant full length VDR [AID392905, Type: Literature]Vitamin D3 receptor [gi:137618]
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26
[SID103221863]
Ki 0.0001Displacement of radiolabeled 1-alpha,25-(OH)2D3 from rat recombinant full length VDR [AID455160, Type: Literature]Vitamin D3 receptor [gi:137618]
View
27
[SID103221863]
EC50 0.0002Activity at VDR in rat ROS 17/2.8 cells assessed as transcriptional activation of 24-hydroxylase gene promoter after 16 hrs by luciferase reporter gene assay [AID392907, Type: Literature]Vitamin D3 receptor [gi:137618]
View
28
[SID103221863]
EC50 0.0002Activity at rat recombinant full length VDR expressed in rat ROS 17/2.8 cells transfected with 24-hydroxylase gene promoter assessed as transcriptional activation after 16 hrs by luciferase reporter gene assay [AID387116, Type: Literature]Vitamin D3 receptor [gi:137618]
View
29
[SID103221863]
ED50 0.0002Inhibition of VDR-induced 24-hydroxylase transcription in rat osteosarcoma cells after 16 hrs by luciferase reporter gene assay [AID672800, Type: Literature]Vitamin D3 receptor [gi:137618]
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30
[SID103221863]
ED50 0.0002Induction of VDR-mediated 24-hydroxylase transcription in rat osteosarcoma cells by luciferase reporter gene assay [AID619491, Type: Literature]Vitamin D3 receptor [gi:137618]
View
31
[SID103221863]
EC50 0.0002Agonist activity at rat VDR in ROS 17/2.8 cells transfected with Cyp24a1 reporter plasmid assessed as increase in Cyp24a1 transcription after 16 hrs by luciferase reporter gene assay [AID635522, Type: Literature]Vitamin D3 receptor [gi:137618]
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32
[SID103221863]
ED50 0.0002Activity at VDR in rat osteosarcoma 17/2.8 cells assessed as transcriptional activation of 24-hydroxylase gene promoter after 16 hrs by luciferase reporter gene assay [AID351853, Type: Literature]Vitamin D3 receptor [gi:137618]
View
33
[SID103221863]
EC50 0.0002Activity at VDR in rat osteosarcoma cells assessed as 24-hydroxylase transcription by reporter gene assay [AID303411, Type: Literature]Vitamin D3 receptor [gi:137618]
View
34
[SID103221863]
Ki 0.0002Activity at rat recombinant full length VDR expressed in rat ROS 17/2.8 cells transfected with 24-hydroxylase gene promoter assessed as transcriptional activation after 16 hrs by luciferase reporter gene assay [AID547391, Type: Literature]Vitamin D3 receptor [gi:137618]
View
35
[SID103221863]
EC50 0.0003Activity at VDR in rat osteosarcoma cells assessed as induction of 24-hydroxylase reporter gene transcription by luciferase reporter gene assay [AID455164, Type: Literature]Vitamin D3 receptor [gi:137618]
View
36
[SID103221863]
ED50 0.00036In vitro vitamin D receptor (VDR)-mediated transcriptional potency in rat osteosarcoma ROS 17/2.8 cells [AID166890, Type: Literature]
View
37
[SID103221863]
ED50 0.0004In vitro vitamin D receptor-mediated antiproliferative activity in rat osteosarcoma ROS 17/2.8 cells [AID228001, Type: Literature]Vitamin D3 receptor [gi:137618]
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38
[SID103221863]
EC50 0.0005Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay [AID326338, Type: Literature]Vitamin D3 receptor [gi:137617]
View
39
[SID103221863]
ED50 0.0005Stabilization of human [35S]VDR against trypsin digestion by protease assay [AID274536, Type: Literature]Vitamin D3 receptor [gi:137617]
View
40
[SID103221863]
EC50 0.0005Induction of transactivation of human VDR responsive gene in COS7 cells by rat osteopontin luciferase reporter gene assay [AID280115, Type: Literature]Vitamin D3 receptor [gi:137617]
View
41
[SID103221863]
ED50 0.0005Stabilization of human [35S]VDR against trypsin digestion by protease assay [AID274536, Type: Literature]Vitamin D3 receptor [gi:137617]
View
42
[SID103221863]
EC50 0.0005Induction of transactivation of human VDR responsive gene in COS7 cells by rat osteopontin luciferase reporter gene assay [AID280115, Type: Literature]Vitamin D3 receptor [gi:137617]
View
43
[SID103221863]
EC50 0.0005Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay [AID326338, Type: Literature]Vitamin D3 receptor [gi:137617]
View
44
[SID103221863]
EC50 0.0005Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay [AID326338, Type: Literature]Vitamin D3 receptor [gi:137617]
View
45
[SID103221863]
ED50 0.0005Stabilization of human [35S]VDR against trypsin digestion by protease assay [AID274536, Type: Literature]Vitamin D3 receptor [gi:137617]
View
46
[SID103221863]
EC50 0.0005Induction of transactivation of human VDR responsive gene in COS7 cells by rat osteopontin luciferase reporter gene assay [AID280115, Type: Literature]Vitamin D3 receptor [gi:137617]
View
47
[SID103221863]
ED50 0.0005Stabilization of human [35S]VDR against trypsin digestion by protease assay [AID274536, Type: Literature]Vitamin D3 receptor [gi:137617]
View
48
[SID103221863]
EC50 0.0005Induction of transactivation of human VDR responsive gene in COS7 cells by rat osteopontin luciferase reporter gene assay [AID280115, Type: Literature]Vitamin D3 receptor [gi:137617]
View
49
[SID103221863]
EC50 0.0005Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay [AID326338, Type: Literature]Vitamin D3 receptor [gi:137617]
View
50
[SID103221863]
IC50 0.00052Antiproliferative activity against mouse SVEC cells assessed as decrease in cell number after 72 hrs by WST assay [AID652549, Type: other]
View