Activity (functional)
|
= -15.2 %
|
Change in body weight of mice on day 14 following per oral administration at 30 mg/kg, twice a day; n = 12; body weight at day 0 = 45 g
|
ChEMBL.
|
15743174
|
Activity (functional)
|
= -15.2 %
|
Change in body weight of mice on day 14 following per oral administration at 30 mg/kg, twice a day; n = 12; body weight at day 0 = 45 g
|
ChEMBL.
|
15743174
|
Activity (functional)
|
= -8.25 %
|
Change in body weight of mice on day 14 following per oral administration at 10 mg/kg, twice a day; n = 12; body weight at day 0 = 44.7 g
|
ChEMBL.
|
15743174
|
Activity (functional)
|
= -8.25 %
|
Change in body weight of mice on day 14 following per oral administration at 10 mg/kg, twice a day; n = 12; body weight at day 0 = 44.7 g
|
ChEMBL.
|
15743174
|
Activity (functional)
|
= 10 ug/g
|
End-of-study drug concentration in inactin-anesthetized Sprague-Dawley rat brain
|
ChEMBL.
|
16570930
|
Activity (functional)
|
= 23 uM
|
End-of-study drug concentration in inactin-anesthetized Sprague-Dawley rat plasma
|
ChEMBL.
|
16570930
|
AUC (ADMET)
|
= 1.33 ug hr-1 g-1
|
Area under concentration time curve in brain of mice following peroral administration of the compound at 10 mg/kg; n=3
|
ChEMBL.
|
15743174
|
AUC (ADMET)
|
= 2.12 ug hr-1 g-1
|
Area under concentration time curve in plasma of mice following peroral administration of the compound at 10 mg/kg; n=3
|
ChEMBL.
|
15743174
|
AUC (ADMET)
|
= 1.33 ug hr-1 ml-1
|
Area under curve of the compound was determined in in diet-induced obese mice brain at 10 mg/kg (p.o.) concentration
|
ChEMBL.
|
15911251
|
AUC (ADMET)
|
= 2.12 ug hr-1 ml-1
|
Area under curve of the compound was determined in in diet-induced obese mice plasma at 10 mg/kg (p.o.) concentration
|
ChEMBL.
|
15911251
|
Body weight (functional)
|
= 39.7 g
|
Body weight of mice on day 14 following per oral administration at 30 mg/kg, twice a day; n = 12
|
ChEMBL.
|
15743174
|
Body weight (functional)
|
= 39.7 g
|
Body weight of mice on day 14 following per oral administration at 30 mg/kg, twice a day; n = 12
|
ChEMBL.
|
15743174
|
Body weight (functional)
|
= 42.6 g
|
Body weight of mice on day 14 following per oral administration at 10 mg/kg, twice a day; n = 12
|
ChEMBL.
|
15743174
|
Body weight (functional)
|
= 42.6 g
|
Body weight of mice on day 14 following per oral administration at 10 mg/kg, twice a day; n = 12
|
ChEMBL.
|
15743174
|
Cmax (ADMET)
|
= 29 ng g-1
|
Maximum concentration of the compound in brain of mice at 12 hours following peroral administration at 10 mg/kg; n=3
|
ChEMBL.
|
15743174
|
Cmax (ADMET)
|
= 177 ng g-1
|
Maximum concentration of the compound in brain of mice following peroral administration at 10 mg/kg; n=3
|
ChEMBL.
|
15743174
|
Cmax (ADMET)
|
= 177 ng g-1
|
Maximum brain compound (10mg/kg, p.o.) concentration in diet-induced obese mice
|
ChEMBL.
|
15911251
|
Cmax (ADMET)
|
= 0.39 ng ml-1
|
Concentration of the compound in plasma of mice,17 hours after administration of final dose at 10 mg/kg, twice a day
|
ChEMBL.
|
15743174
|
Cmax (ADMET)
|
= 2.23 ng ml-1
|
Concentration of the compound in plasma of mice,17 hours after administration of final dose at 30 mg/kg, twice a day
|
ChEMBL.
|
15743174
|
Cmax (ADMET)
|
= 5.35 ng ml-1
|
Concentration of the compound in brain of mice,17 hours after administration of final dose at 30 mg/kg, twice a day
|
ChEMBL.
|
15743174
|
Cmax (ADMET)
|
= 7.02 ng ml-1
|
Concentration of the compound in brain of mice,17 hours after administration of final dose at 10 mg/kg, twice a day
|
ChEMBL.
|
15743174
|
Cmax (ADMET)
|
= 115 ng ml-1
|
Concentration of the compound in brain of mice,1 hour after administration of final dose at 10 mg/kg, twice a day
|
ChEMBL.
|
15743174
|
Cmax (ADMET)
|
= 168 ng ml-1
|
Concentration of the compound in plasma of mice,1 hour after administration of final dose at 10 mg/kg, twice a day
|
ChEMBL.
|
15743174
|
Cmax (ADMET)
|
= 233 ng ml-1
|
Concentration of the compound in brain of mice,1 hour after administration of final dose at 30 mg/kg, twice a day
|
ChEMBL.
|
15743174
|
Cmax (ADMET)
|
= 596 ng ml-1
|
Maximum plasma compound (10mg/kg, p.o.) concentration in diet-induced obese mice
|
ChEMBL.
|
15911251
|
Cmax (ADMET)
|
= 824 ng ml-1
|
Concentration of the compound in plasma of mice,1 hour after administration of final dose at 30 mg/kg, twice a day
|
ChEMBL.
|
15743174
|
IC50 (binding)
|
= 1.4 nM
|
Inihibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
|
ChEMBL.
|
15743174
|
IC50 (binding)
|
= 1.4 nM
|
Inhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese mice
|
ChEMBL.
|
15911251
|
IC50 (binding)
|
= 1.4 nM
|
Displacement of [125I]-MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
|
ChEMBL.
|
16570930
|
IC50 (binding)
|
= 1.4 nM
|
Inihibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
|
ChEMBL.
|
15743174
|
IC50 (binding)
|
= 1.4 nM
|
Inhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese mice
|
ChEMBL.
|
15911251
|
IC50 (binding)
|
= 1.4 nM
|
Displacement of [125I]-MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
|
ChEMBL.
|
16570930
|
IC50 (binding)
|
= 1.4 nM
|
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
|
ChEMBL.
|
21190859
|
IC50 (functional)
|
= 11 nM
|
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR assay
|
ChEMBL.
|
16570930
|
IC50 (functional)
|
= 11 nM
|
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR assay
|
ChEMBL.
|
16570930
|
IC50 (functional)
|
= 0.011 uM
|
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
|
ChEMBL.
|
15743174
|
IC50 (functional)
|
= 0.011 uM
|
Inhibition of Melanin-concentrating hormone (MCH) mediated [Ca2+] release in IMR-32 cells
|
ChEMBL.
|
15911251
|
IC50 (functional)
|
= 0.011 uM
|
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
|
ChEMBL.
|
15743174
|
IC50 (functional)
|
= 0.011 uM
|
Inhibition of Melanin-concentrating hormone (MCH) mediated [Ca2+] release in IMR-32 cells
|
ChEMBL.
|
15911251
|