Activity (functional)
|
0
|
Fracture incidence in rat at low dose; 0/8
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Fracture incidence in rat at mid dose 1; 0/8
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Fracture incidence in rat at mid dose 2; 4/8
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Fracture incidence in rat at high dose; 3/8
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 0
|
Average number of fractures per rat at low dose
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 0
|
Average number of fractures per rat at mid dose 1
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Skin scaling in mice at low dose with Hypervitaminosis; 0/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Skin scaling in mice at mid dose 1 with Hypervitaminosis; 0/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Skin scaling in mice at mid dose 2 with Hypervitaminosis; 0/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Skin scaling in mice at high dose with Hypervitaminosis; 2/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Alopecia in mice observed at low dose with Hypervitaminosis; 0/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Alopecia in mice observed at mid dose 1 with Hypervitaminosis; 2/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Alopecia in mice observed at mid dose 2 with Hypervitaminosis; 3/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Alopecia in mice observedat high dose with Hypervitaminosis; 4/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Avoiding pressure on limbs in mice at low dose with Hypervitaminosis; 0/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Avoiding pressure on limbs in mice at mid dose 1 with Hypervitaminosis 0/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Avoiding pressure on limbs in mice at mid dose 2 with Hypervitaminosis; 0/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Avoiding pressure on limbs in mice at high dose with with Hypervitaminosis; 4/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Enlarged spleen in Gross pathological observations in mice with hypervitaminosis A at low dose with gross observations/total number of mice in group; 0/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Enlarged spleen in Gross pathological observations in mice with hypervitaminosis A at mid dose 1 with gross observations/total number of mice in group; 1/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Enlarged spleen in Gross pathological observations in mice with hypervitaminosis A at mid dose 1 with gross observations/total number of mice in group; 0/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Enlarged spleen in Gross pathological observations in mice with hypervitaminosis A at high dose with gross observations/total number of mice in group; 0/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Enlarged lymph in gross pathological observations in mice with hypervitaminosis A at low dose with gross observations/total number of mice in group; 1/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Enlarged lymph in gross pathological observations in mice with hypervitaminosis A at mid dose 1 with gross observations/total number of mice in group; 2/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Enlarged lymph in gross pathological observations in mice with hypervitaminosis A at mid dose 2 with gross observations/total number of mice in group; 1/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Enlarged lymph in gross pathological observations in mice with hypervitaminosis A in mice at high dose with gross observations/total number of mice in group; 1/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 0.3
|
Effect of compound on adrenal to body weight ratios in mice at low dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 0.3
|
Effect of compound on adrenal to body weight ratios in mice at mid dose 1 on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 0.3
|
Effect of compound on adrenal to body weight ratios in mice at mid dose 2 on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 0.4
|
Effect of compound on adrenal to body weight ratios in mice at high dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 0.6
|
Average number of fractures per rat at mid dose 2
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 1
|
Average number of fractures per rat at high dose
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 1.3
|
Effect of compound on thymus to body weight ratios in mice at high dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 1.5
|
Effect of compound on thymus to body weight ratios in mice at mid dose 2 on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 1.6
|
Effect of compound on thymus to body weight ratios in mice at low dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 1.6
|
Effect of compound on thymus to body weight ratios in mice at mid dose 1 on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 2.3
|
Effect of compound on Spleen to body weight ratios in mice at low dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 2.5
|
Effect of compound on Spleen to body weight ratios in mice at mid dose 1 on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 2.7
|
Effect of compound on Spleen to body weight ratios in mice at mid dose 2 on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 2.9
|
Effect of compound on right testicle to body weight ratios in mice at mid dose 1 on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 3
|
Effect of compound on right testicle to body weight ratios in mice at high dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 3
|
Effect of compound on Spleen to body weight ratios in mice at high dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 3.2
|
Effect of compound on right testicle to body weight ratios in mice at low dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 3.3
|
Effect of compound on right testicle to body weight ratios in mice at mid dose 2 on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 3.7
|
Effect of compound on white blood cells levels in mice at high dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 4.51
|
Effect of compound on white blood cells levels in mice at mid dose 2 on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 4.84
|
Effect of compound on white blood cells levels in mice at low dose on day 8
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 53
|
Approximate day to 10% weight loss in mice at high dose
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 61
|
Approximate day to 10% weight loss in mice at mid dose 2
|
ChEMBL.
|
9357524
|
Activity (functional)
|
> 65
|
Approximate day to 10% weight loss in mice at low dose
|
ChEMBL.
|
9357524
|
Activity (functional)
|
> 65
|
Approximate day to 10% weight loss in mice at mid dose 1
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 91.9
|
Effect of compound on serum Alkaline phosphatase levels in mice at high dose on day 36
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 96.8
|
Effect of compound on serum triglycerides levels in mice at low dose on day 8
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 96.8
|
Effect of compound on serum Alkaline phosphatase levels in mice at low dose on day 29
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 97.2
|
Effect of compound on serum triglycerides levels in mice at mid dose 1 on day 8
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 112.3
|
Effect of compound on serum triglycerides levels in mice at mid dose 2 on day 8
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 115.7
|
Effect of compound on serum Alkaline phosphatase levels in mice at low dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 127.1
|
Effect of compound on serum Alkaline phosphatase levels in mice at mid dose 1 on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 136.8
|
Effect of compound on serum Alkaline phosphatase levels in mice at mid dose 2 on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 156.8
|
Effect of compound on serum Alkaline phosphatase levels in mice at high dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 159.3
|
Effect of compound on serum triglycerides levels in mice at mid dose 2 on day 29
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 167.3
|
Effect of compound on serum triglycerides levels in mice at mid dose 1 on day 29
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 179.4
|
Effect of compound on serum triglycerides levels in mice at low dose on day 29
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 187.1
|
Effect of compound on serum triglycerides levels in mice at low dose on day 36
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 195.9
|
Effect of compound on serum triglycerides levels in mice at mid dose 2 on day 36
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 202.8
|
Effect of compound on serum triglycerides levels in mice at mid dose 1 on day 36
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 208.2
|
Effect of compound on serum triglycerides levels in mice at high dose on day 29
|
ChEMBL.
|
9357524
|
Dose (functional)
|
> 207.1 mg kg-1
|
Total dose of 10% weight loss in mice at low dose
|
ChEMBL.
|
9357524
|
Dose (functional)
|
> 207.1 mg kg-1
|
Total dose of 10% weight loss in mice at low dose
|
ChEMBL.
|
9357524
|
Dose (functional)
|
> 414.2 mg kg-1
|
Total dose of 10% weight loss in mice at mid dose 1
|
ChEMBL.
|
9357524
|
Dose (functional)
|
> 414.2 mg kg-1
|
Total dose of 10% weight loss in mice at mid dose 1
|
ChEMBL.
|
9357524
|
Dose (functional)
|
= 732.4 mg kg-1
|
Total dose of 10% weight loss in mice at mid dose 2
|
ChEMBL.
|
9357524
|
Dose (functional)
|
= 732.4 mg kg-1
|
Total dose of 10% weight loss in mice at mid dose 2
|
ChEMBL.
|
9357524
|
Dose (functional)
|
= 952.8 mg kg-1
|
Total dose of 10% weight loss in mice at high dose
|
ChEMBL.
|
9357524
|
Dose (functional)
|
= 952.8 mg kg-1
|
Total dose of 10% weight loss in mice at high dose
|
ChEMBL.
|
9357524
|
EC50 (binding)
|
= 39 nM
|
Transcriptional activation in CV-1 cells expressing RAR-gamma receptor
|
ChEMBL.
|
9733501
|
EC50 (binding)
|
= 39 nM
|
Transcriptional activation in CV-1 cells expressing RAR-gamma receptor
|
ChEMBL.
|
9733501
|
EC50 (binding)
|
= 72 nM
|
Transcriptional activation in CV-1 cells expressing RAR-beta receptor
|
ChEMBL.
|
9733501
|
EC50 (binding)
|
= 72 nM
|
Transcriptional activation in CV-1 cells expressing RAR-beta receptor
|
ChEMBL.
|
9733501
|
EC50 (binding)
|
= 740 nM
|
Transcriptional activation in CV-1 cells expressing RAR-alpha receptor
|
ChEMBL.
|
9733501
|
EC50 (binding)
|
= 740 nM
|
Transcriptional activation in CV-1 cells expressing RAR-alpha receptor
|
ChEMBL.
|
9733501
|
EC50 (binding)
|
= 2800 nM
|
Transcriptional activation in CV-1 cells expressing RAR-alpha receptor
|
ChEMBL.
|
9733501
|
EC50 (binding)
|
= 2800 nM
|
Transcriptional activation in CV-1 cells expressing RAR-alpha receptor
|
ChEMBL.
|
9733501
|
Inhibition (functional)
|
= 74 %
|
Inhibition of TPA induced ODC(Ornithine decarboxylase) activity in mice epidermis at 34 nmol in the presence of TPA compared to control value
|
ChEMBL.
|
3612691
|
Inhibition (functional)
|
= 74 %
|
Inhibition of TPA induced ODC(Ornithine decarboxylase) activity in mice epidermis at 34 nmol in the presence of TPA compared to control value
|
ChEMBL.
|
3612691
|
Max tolerated dose (functional)
|
> 6.9 mg kg-1
|
Calculated 30-day maximally tolerated dose based on 10% weight loss in mice at low dose
|
ChEMBL.
|
9357524
|
Max tolerated dose (functional)
|
> 6.9 mg kg-1
|
Calculated 30-day maximally tolerated dose based on 10% weight loss in mice at low dose
|
ChEMBL.
|
9357524
|
Max tolerated dose (functional)
|
> 13.8 mg kg-1
|
Calculated 30-day maximally tolerated dose based on 10% weight loss in mice at mid dose 1
|
ChEMBL.
|
9357524
|
Max tolerated dose (functional)
|
> 13.8 mg kg-1
|
Calculated 30-day maximally tolerated dose based on 10% weight loss in mice at mid dose 1
|
ChEMBL.
|
9357524
|
Max tolerated dose (functional)
|
= 24.4 mg kg-1
|
Calculated 30-day maximally tolerated dose based on 10% weight loss in mice at mid dose 2
|
ChEMBL.
|
9357524
|
Max tolerated dose (functional)
|
= 24.4 mg kg-1
|
Calculated 30-day maximally tolerated dose based on 10% weight loss in mice at mid dose 2
|
ChEMBL.
|
9357524
|
Max tolerated dose (functional)
|
= 31.8 mg kg-1
|
Calculated 30-day maximally tolerated dose based on 10% weight loss in mice at high dose
|
ChEMBL.
|
9357524
|
Max tolerated dose (functional)
|
= 31.8 mg kg-1
|
Calculated 30-day maximally tolerated dose based on 10% weight loss in mice at high dose
|
ChEMBL.
|
9357524
|
Mortality (functional)
|
= 0 day of death
|
Mortality rate of the compound in mice in low dose
|
ChEMBL.
|
9357524
|
Mortality (functional)
|
= 0 day of death
|
Mortality rate of the compound in mice in mid dose 1
|
ChEMBL.
|
9357524
|
Mortality (functional)
|
= 0 day of death
|
Mortality rate of the compound in mice in mid dose 2
|
ChEMBL.
|
9357524
|
Mortality (functional)
|
= 0 day of death
|
Mortality rate of the compound in mice in high dose
|
ChEMBL.
|
9357524
|
Mortality (functional)
|
= 0 day of death
|
Mortality rate of the compound in mice in low dose
|
ChEMBL.
|
9357524
|
Mortality (functional)
|
= 0 day of death
|
Mortality rate of the compound in mice in mid dose 1
|
ChEMBL.
|
9357524
|
Mortality (functional)
|
= 0 day of death
|
Mortality rate of the compound in mice in mid dose 2
|
ChEMBL.
|
9357524
|
Mortality (functional)
|
= 0 day of death
|
Mortality rate of the compound in mice in high dose
|
ChEMBL.
|
9357524
|
ODC activity (functional)
|
= 1.4 (nM of CO2) hr-1 (mg of protein)-1
|
Inhibition of TPA induced ODC(Ornithine decarboxylase) activity in mice epidermis at 34 nmol in the presence of TPA
|
ChEMBL.
|
3612691
|
ODC activity (functional)
|
= 1.4 (nM of CO2) hr-1 (mg of protein)-1
|
Inhibition of TPA induced ODC(Ornithine decarboxylase) activity in mice epidermis at 34 nmol in the presence of TPA
|
ChEMBL.
|
3612691
|
Relative activity (functional)
|
= 50
|
Relative transcriptional activation activity of the compound relative to t-RA
|
ChEMBL.
|
9357524
|
Total dose (functional)
|
= 207.1 mg kg-1
|
Compound total dose to termination (day 25/65) in low dose
|
ChEMBL.
|
9357524
|
Total dose (functional)
|
= 207.1 mg kg-1
|
Compound total dose to termination (day 25/65) in low dose
|
ChEMBL.
|
9357524
|
Total dose (functional)
|
= 414.2 mg kg-1
|
Compound total dose to termination (day 25/65) in mid dose 1
|
ChEMBL.
|
9357524
|
Total dose (functional)
|
= 414.2 mg kg-1
|
Compound total dose to termination (day 25/65) in mid dose 1
|
ChEMBL.
|
9357524
|
Total dose (functional)
|
= 828.4 mg kg-1
|
Compound total dose to termination (day 25/65) in mid dose 2
|
ChEMBL.
|
9357524
|
Total dose (functional)
|
= 828.4 mg kg-1
|
Compound total dose to termination (day 25/65) in mid dose 2
|
ChEMBL.
|
9357524
|
Total dose (functional)
|
= 3106.5 mg kg-1
|
Compound total dose to termination (day 25/65) in high dose
|
ChEMBL.
|
9357524
|
Total dose (functional)
|
= 3106.5 mg kg-1
|
Compound total dose to termination (day 25/65) in high dose
|
ChEMBL.
|
9357524
|