Activity (functional)
|
= 18.4 %
|
Lowering of intraocular pressure in lasered cynomolgus monkey after 1 hr at 300 ug
|
ChEMBL.
|
16392816
|
Activity (functional)
|
= 18.4 %
|
Lowering of intraocular pressure in lasered cynomolgus monkey after 1 hr at 300 ug
|
ChEMBL.
|
16392816
|
Activity (functional)
|
= 30.8 %
|
Lowering of intraocular pressure in lasered cynomolgus monkey after 3 hrs at 300 ug
|
ChEMBL.
|
16392816
|
Activity (functional)
|
= 30.8 %
|
Lowering of intraocular pressure in lasered cynomolgus monkey after 3 hrs at 300 ug
|
ChEMBL.
|
16392816
|
Activity (functional)
|
= 32.7 %
|
Lowering of intraocular pressure in lasered cynomolgus monkey after 6 hrs at 300 ug
|
ChEMBL.
|
16392816
|
Activity (functional)
|
= 32.7 %
|
Lowering of intraocular pressure in lasered cynomolgus monkey after 6 hrs at 300 ug
|
ChEMBL.
|
16392816
|
EC50 (functional)
|
= 4.9 nM
|
Activity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cells
|
ChEMBL.
|
16392816
|
EC50 (functional)
|
= 4.9 nM
|
Activity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cells
|
ChEMBL.
|
16392816
|
EC50 (functional)
|
= 5.9 nM
|
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
|
ChEMBL.
|
16392816
|
EC50 (functional)
|
= 5.9 nM
|
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
|
ChEMBL.
|
16392816
|
EC50 (functional)
|
= 59.7 nM
|
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
|
ChEMBL.
|
16392816
|
EC50 (functional)
|
= 59.7 nM
|
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
|
ChEMBL.
|
16392816
|
ED5 (functional)
|
= 0.56 mg kg-1
|
Head twitch response in SD mice, sc
|
ChEMBL.
|
16392816
|
ED5 (functional)
|
= 0.56 mg kg-1
|
Head twitch response in SD mice, sc
|
ChEMBL.
|
16392816
|
Emax (functional)
|
= 87 %
|
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
|
ChEMBL.
|
16392816
|
Emax (functional)
|
= 87 %
|
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
|
ChEMBL.
|
16392816
|
Emax (functional)
|
= 104 %
|
Activity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cells
|
ChEMBL.
|
16392816
|
Emax (functional)
|
= 104 %
|
Activity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cells
|
ChEMBL.
|
16392816
|
IC50 (binding)
|
= 0.54 nM
|
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
|
ChEMBL.
|
16392816
|
IC50 (binding)
|
= 0.54 nM
|
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
|
ChEMBL.
|
16392816
|
Ki (binding)
|
= 1.2 nM
|
Displacement of [125I]DOI from cloned human 5HT2C receptor expressed in CHO cells
|
ChEMBL.
|
16392816
|
Ki (binding)
|
= 1.2 nM
|
Displacement of [125I]DOI from cloned human 5HT2C receptor expressed in CHO cells
|
ChEMBL.
|
16392816
|
Ki (binding)
|
= 3.8 nM
|
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
|
ChEMBL.
|
16392816
|
Ki (binding)
|
= 3.8 nM
|
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
|
ChEMBL.
|
16392816
|
Ki (binding)
|
= 12 nM
|
Displacement of [125I]DOI from cloned human 5HT2A receptor expressed in CHO cells
|
ChEMBL.
|
16392816
|
Ki (binding)
|
= 12 nM
|
Displacement of [125I]DOI from cloned human 5HT2A receptor expressed in CHO cells
|
ChEMBL.
|
16392816
|
Log D |
= 1.09
|
Distribution coefficient at pH 7.4
|
ChEMBL.
|
16392816
|
Papp (ADMET)
|
= 13.6 nM/s
|
Passive diffusion permeability from apical to basolateral side of the MDCK cell transfected with human MDR1 in presence of cyclosporin A
|
ChEMBL.
|
16392816
|
Papp (ADMET)
|
= 16.5 nM/s
|
Permeability from apical to basolateral side of the MDCK cell transfected with human MDR1
|
ChEMBL.
|
16392816
|
Papp (ADMET)
|
= 32.5 nM/s
|
Passive diffusion permeability from basolateral to apical side of the MDCK cell transfected with human MDR1 in presence of cyclosporin A
|
ChEMBL.
|
16392816
|
Papp (ADMET)
|
= 49.4 nM/s
|
Permeability from basolateral to apical side of the MDCK cell transfected with human MDR1
|
ChEMBL.
|
16392816
|
Ratio (ADMET)
|
= 2.4
|
Ratio of passive diffusion permeability from basolateral to apical over apical to basolateral side of the MDCK cell transfected with MDR1 in presence of cyclosporin A
|
ChEMBL.
|
16392816
|
Ratio (ADMET)
|
= 3
|
Ratio of permeability from basolateral to apical over apical to basolateral side of the MDCK cell transfected with human MDR1
|
ChEMBL.
|
16392816
|
T1/2 (ADMET)
|
= 4 yr
|
Half life in phosphate buffer at pH 7.4 in 25 degC
|
ChEMBL.
|
16392816
|