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; 0/8
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Fracture incidence in rat at high dose; 2/8
|
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 lmid dose 1
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 0
|
Average number of fractures per rat at mid dose 2
|
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; 1/16
|
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; 0/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Alopecia in mice observed at low dose with Hypervitaminosis; 1/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Alopecia in mice observed at mid dose 1 with Hypervitaminosis; 1/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Alopecia in mice observed at mid dose 2 with Hypervitaminosis; 1/16
|
ChEMBL.
|
9357524
|
Activity (functional)
|
0
|
Alopecia in mice observedat high dose with Hypervitaminosis; 1/16
|
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 Hypervitaminosis; 0/16
|
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; 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; 0/16
|
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; 2/16
|
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
|
Average number of fractures per rat at high dose
|
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)
|
= 1.5
|
Effect of compound on thymus to body weight ratios in mice at mid dose 1 on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 1.5
|
Effect of compound on thymus to body weight ratios in mice at high dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 1.6
|
Effect of compound on thymus to body weight ratios in mice at mid dose 2 on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 1.7
|
Effect of compound on thymus to body weight ratios in mice at low dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 2
|
Effect of compound on Spleen to body weight ratios in mice at mid dose 1 on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 2.1
|
Effect of compound on Spleen to body weight ratios in mice at low dose
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 2.2
|
Effect of compound on Spleen to body weight ratios in mice at mid dose 2 on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 2.6
|
Effect of compound on right testicle to body weight ratios in mice at low dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 2.6
|
Effect of compound on Spleen to body weight ratios in mice at high dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 2.6
|
Effect of compound on adrenal to body weight ratios in mice at high dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 2.7
|
Effect of compound on right testicle to body weight ratios in mice at high dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 2.8
|
Effect of compound on right testicle to body weight ratios in mice at mid dose 2 on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 3.1
|
Effect of compound on right testicle to body weight ratios in mice at mid dose 1 on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 4.18
|
Effect of compound on white blood cells levels in mice at high dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 54
|
Approximate day to 10% weight loss in mice at high dose
|
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)
|
> 65
|
Approximate day to 10% weight loss in mice at mid dose 2
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 75.6
|
Effect of compound on serum Alkaline phosphatase levels in mice at mid dose 2 on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 84.6
|
Effect of compound on serum Alkaline phosphatase levels in mice at high dose on day 36
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 94.6
|
Effect of compound on serum Alkaline phosphatase levels in mice at high dose on day 29
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 94.9
|
Effect of compound on serum Alkaline phosphatase levels in mice at low dose on day 29
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 97.5
|
Effect of compound on serum triglycerides levels in mice at low dose on day 8
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 97.6
|
Effect of compound on serum triglycerides levels in mice at mid dose 1 on day 8
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 127.5
|
Effect of compound on serum Alkaline phosphatase levels in mice at low dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 135.8
|
Effect of compound on serum Alkaline phosphatase levels in mice at mid dose 1 on day 29
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 136.8
|
Effect of compound on serum Alkaline phosphatase levels in mice at mid dose 2 on day 36
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 153.4
|
Effect of compound on serum triglycerides levels in mice at mid dose 2 on day 29
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 159
|
Effect of compound on serum Alkaline phosphatase levels in mice at high dose on day 65
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 164.2
|
Effect of compound on serum triglycerides levels in mice at high dose on day 29
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 174.1
|
Effect of compound on serum triglycerides levels in mice at mid dose 1 on day 29
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 176.4
|
Effect of compound on serum triglycerides levels in mice at low dose on day 29
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 194.9
|
Effect of compound on serum triglycerides levels in mice at low dose on day 36
|
ChEMBL.
|
9357524
|
Activity (functional)
|
= 212.7
|
Effect of compound on serum triglycerides levels in mice at mid dose 1 on day 36
|
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)
|
> 828.4 mg kg-1
|
Total dose of 10% weight loss in mice at mid dose 2
|
ChEMBL.
|
9357524
|
Dose (functional)
|
> 828.4 mg kg-1
|
Total dose of 10% weight loss in mice at mid dose 2
|
ChEMBL.
|
9357524
|
Dose (functional)
|
= 1016.8 mg kg-1
|
Total dose of 10% weight loss in mice at high dose
|
ChEMBL.
|
9357524
|
Dose (functional)
|
= 1016.8 mg kg-1
|
Total dose of 10% weight loss in mice at high dose
|
ChEMBL.
|
9357524
|
EC50 (binding)
|
= 12 nM
|
Transcriptional activation in CV-1 cells expressing RAR-gamma receptor
|
ChEMBL.
|
9733501
|
EC50 (binding)
|
= 12 nM
|
Transcriptional activation in CV-1 cells expressing RAR-gamma receptor
|
ChEMBL.
|
9733501
|
EC50 (binding)
|
= 43 nM
|
Transcriptional activation in CV-1 cells expressing RAR-beta receptor
|
ChEMBL.
|
9733501
|
EC50 (binding)
|
= 43 nM
|
Transcriptional activation in CV-1 cells expressing RAR-beta receptor
|
ChEMBL.
|
9733501
|
EC50 (binding)
|
= 1400 nM
|
Transcriptional activation in CV-1 cells expressing RAR-alpha receptor
|
ChEMBL.
|
9733501
|
EC50 (binding)
|
= 1400 nM
|
Transcriptional activation in CV-1 cells expressing RAR-alpha receptor
|
ChEMBL.
|
9733501
|
EC50 (binding)
|
= 2700 nM
|
Transcriptional activation in CV-1 cells expressing RAR-alpha receptor
|
ChEMBL.
|
9733501
|
EC50 (binding)
|
= 2700 nM
|
Transcriptional activation in CV-1 cells expressing RAR-alpha receptor
|
ChEMBL.
|
9733501
|
ED50 (functional)
|
= 500 nM
|
Compound was evaluated for the retinoid-induced differentiation of the human myeloid leukemia cell line HL-60 using trans-retinoic acid as the standard.
|
ChEMBL.
|
1992144
|
ED50 (functional)
|
= 500 nM
|
Compound was evaluated for the retinoid-induced differentiation of the human myeloid leukemia cell line HL-60 using trans-retinoic acid as the standard.
|
ChEMBL.
|
1992144
|
ID50 (functional)
|
= 3.3 nM
|
Compound was evaluated for the ability to inhibit the phorbol ester induced increase of mouse epidermal ornithine decarboxylase (ODC) activity by 50% when administered topically using ODC assay.
|
ChEMBL.
|
1992144
|
ID50 (functional)
|
= 3.3 nM
|
Compound was evaluated for the ability to inhibit the phorbol ester induced increase of mouse epidermal ornithine decarboxylase (ODC) activity by 50% when administered topically using ODC assay.
|
ChEMBL.
|
1992144
|
Inhibition (functional)
|
= 1 %
|
Inhibition of SCC-38 cell proliferation
|
ChEMBL.
|
10543887
|
Inhibition (functional)
|
= 1 %
|
Inhibition of SCC-38 cell proliferation
|
ChEMBL.
|
10543887
|
Inhibition (functional)
|
= 2 %
|
Inhibition of SCC-2 cell proliferation
|
ChEMBL.
|
10543887
|
Inhibition (functional)
|
= 89 %
|
Inhibition of TPA induced ODC(Ornithine decarboxylase) activity in mice epidermis at 17 nmol in the presence of TPA compared to control value
|
ChEMBL.
|
3612691
|
Inhibition (functional)
|
= 89 %
|
Inhibition of TPA induced ODC(Ornithine decarboxylase) activity in mice epidermis at 17 nmol in the presence of 13-cis-retinoic acid + TPA compared to control value
|
ChEMBL.
|
3612691
|
Inhibition (functional)
|
= 89 %
|
Inhibition of TPA induced ODC(Ornithine decarboxylase) activity in mice epidermis at 17 nmol in the presence of TPA compared to control value
|
ChEMBL.
|
3612691
|
Inhibition (functional)
|
= 89 %
|
Inhibition of TPA induced ODC(Ornithine decarboxylase) activity in mice epidermis at 17 nmol in the presence of 13-cis-retinoic acid + 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)
|
> 27.6 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)
|
> 27.6 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)
|
= 33.9 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)
|
= 33.9 mg kg-1
|
Calculated 30-day maximally tolerated dose based on 10% weight loss in mice at high dose
|
ChEMBL.
|
9357524
|
Mortality (ADMET)
|
= 0 day of death
|
Mortality rate of the compound in mice in low dose
|
ChEMBL.
|
9357524
|
Mortality (ADMET)
|
= 0 day of death
|
Mortality rate of the compound in mice in mid dose 2
|
ChEMBL.
|
9357524
|
Mortality (ADMET)
|
= 0 day of death
|
Mortality rate of the compound in mice in high dose
|
ChEMBL.
|
9357524
|
Mortality (ADMET)
|
= 1 day of death
|
Mortality rate of the compound in mice in mid dose 1
|
ChEMBL.
|
9357524
|
ODC activity (functional)
|
= 0 (nM of CO2) 30min-1 (mg of protein)-1
|
Inhibition of TPA induced ODC(Ornithine decarboxylase) activity in mice epidermis at 0 nmol in the presence of acetone
|
ChEMBL.
|
3612691
|
ODC activity (functional)
|
= 0 (nM of CO2) 30min-1 (mg of protein)-1
|
Inhibition of TPA induced ODC(Ornithine decarboxylase) activity in mice epidermis at 0 nmol in the presence of acetone
|
ChEMBL.
|
3612691
|
ODC activity (functional)
|
= 0.1 (nM of CO2) 30min-1 (mg of protein)-1
|
Inhibition of TPA induced ODC(Ornithine decarboxylase) activity in mice epidermis at 17 nmol in the presence of TPA
|
ChEMBL.
|
3612691
|
ODC activity (functional)
|
= 0.1 (nM of CO2) 30min-1 (mg of protein)-1
|
Inhibition of TPA induced ODC(Ornithine decarboxylase) activity in mice epidermis at 17 nmol in the presence of 13-cis-retinoic acid + TPA
|
ChEMBL.
|
3612691
|
ODC activity (functional)
|
= 0.1 (nM of CO2) 30min-1 (mg of protein)-1
|
Inhibition of TPA induced ODC(Ornithine decarboxylase) activity in mice epidermis at 17 nmol in the presence of TPA
|
ChEMBL.
|
3612691
|
ODC activity (functional)
|
= 0.1 (nM of CO2) 30min-1 (mg of protein)-1
|
Inhibition of TPA induced ODC(Ornithine decarboxylase) activity in mice epidermis at 17 nmol in the presence of 13-cis-retinoic acid + TPA
|
ChEMBL.
|
3612691
|
ODC activity (functional)
|
= 0.9 (nM of CO2) 30min-1 (mg of protein)-1
|
Inhibition of TPA induced ODC(Ornithine decarboxylase) activity in mice epidermis at 0 nmol in the presence of acetone + TPA
|
ChEMBL.
|
3612691
|
ODC activity (functional)
|
= 0.9 (nM of CO2) 30min-1 (mg of protein)-1
|
Inhibition of TPA induced ODC(Ornithine decarboxylase) activity in mice epidermis at 0 nmol in the presence of acetone + TPA
|
ChEMBL.
|
3612691
|
Relative activity (functional)
|
= 52
|
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
|