Activity (functional)
|
|
Blocking the inhibitory effect of 1 nM melatonin.
|
ChEMBL.
|
7932550
|
Activity (functional)
|
0
|
Blocking the inhibitory effect of 1 nM melatonin.
|
ChEMBL.
|
7932550
|
cAMP activity index (functional)
|
= 1.45
|
Activity (expressed as cAMP index) measured by the melatonin-mediated inhibition of forskolin-stimulated cAMP production
|
ChEMBL.
|
7932550
|
cAMP activity index (functional)
|
= 1.45
|
Activity (expressed as cAMP index) measured by the melatonin-mediated inhibition of forskolin-stimulated cAMP production
|
ChEMBL.
|
7932550
|
IC50 (binding)
|
= 7.19
|
Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells
|
ChEMBL.
|
18400335
|
IC50 (binding)
|
= 8.8
|
Melatonin receptor type 1A binding affinity measured using 2-[125I]-iodomelatonin on ovine pars tuberalis membrane homogenates.
|
ChEMBL.
|
9804685
|
IC50 (binding)
|
= 0.0000000017 M
|
Monophasic inhibitory concentration against melatonin receptor was measured on ovine pars tuberalis membrane.
|
ChEMBL.
|
7932550
|
IC50 (binding)
|
= 0.0000000017 M
|
Monophasic inhibitory concentration against melatonin receptor was measured on ovine pars tuberalis membrane.
|
ChEMBL.
|
7932550
|
IC50 (binding)
|
= 0.6 nM
|
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
|
ChEMBL.
|
18372181
|
IC50 (binding)
|
= 0.7 nM
|
Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in HEK293 cells
|
ChEMBL.
|
18372181
|
Kd (binding)
|
= 0.000000000859
|
Binding affinity to melatonin receptor measured on ovine pars tuberalis membrane
|
ChEMBL.
|
7932550
|
Kd (binding)
|
= 0.000000000859
|
Binding affinity to melatonin receptor measured on ovine pars tuberalis membrane
|
ChEMBL.
|
7932550
|
Ki (binding)
|
= 0.15 nM
|
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]-iodomelatonin as radioligand.
|
ChEMBL.
|
12061881
|
Ki (binding)
|
= 0.15 nM
|
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]-iodomelatonin as radioligand.
|
ChEMBL.
|
12061881
|
Ki (binding)
|
= 0.15 nM
|
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
|
ChEMBL.
|
26820449
|
Ki (binding)
|
= 0.15 nM
|
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
|
ChEMBL.
|
26785296
|
Ki (binding)
|
= 0.34 nM
|
Binding affinity on human melatonin receptor type 1B stably transfected in human embryonic kidney (HEK 293) cells using 2-[125I]-iodomelatonin as radioligand.
|
ChEMBL.
|
12061881
|
Ki (binding)
|
= 0.34 nM
|
Binding affinity on human melatonin receptor type 1B stably transfected in human embryonic kidney (HEK 293) cells using 2-[125I]-iodomelatonin as radioligand.
|
ChEMBL.
|
12061881
|
Ki (binding)
|
= 0.34 nM
|
Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cell membranes after 120 mins
|
ChEMBL.
|
26820449
|
Ki (binding)
|
= 0.34 nM
|
Displacement of [125I]2-Iodomelatonin from human MT2 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
|
ChEMBL.
|
26785296
|
Log IC50 (binding)
|
= 8.8
|
Melatonin receptor type 1A binding affinity measured using 2-[125I]-iodomelatonin on ovine pars tuberalis membrane homogenates.
|
ChEMBL.
|
9804685
|
pC1 (binding)
|
= 3.469
|
Binding affinity against melatonin receptor type 1B
|
ChEMBL.
|
15177448
|
pC1 (binding)
|
= 3.824
|
Binding affinity against Melatonin receptor type 1A
|
ChEMBL.
|
15177448
|
pC1 (binding)
|
= 3.469
|
Binding affinity against melatonin receptor type 1B
|
ChEMBL.
|
15177448
|
pC1 (binding)
|
= 3.824
|
Binding affinity against Melatonin receptor type 1A
|
ChEMBL.
|
15177448
|
pRA (binding)
|
= -0.97
|
Negative logarithm of relative affinity (pRA) towards melatonin receptor (relative to N-actyl-5-methoxytryptamine (aMT))
|
ChEMBL.
|
9748358
|
pRA (binding)
|
= -0.97
|
Negative logarithm of relative affinity (pRA) towards melatonin receptor (relative to N-actyl-5-methoxytryptamine (aMT))
|
ChEMBL.
|
9748358
|
Ratio (binding)
|
= 0.5
|
Melatonin receptor type 1A/Melatonin receptor type 1B affinity ratio.
|
ChEMBL.
|
12061881
|
Ratio (binding)
|
= 0.5
|
Melatonin receptor type 1A/Melatonin receptor type 1B affinity ratio.
|
ChEMBL.
|
12061881
|
Selectivity (binding)
|
= -0.355
|
Selectivity of the compound (pC2-PC1) was determined
|
ChEMBL.
|
15177448
|
Selectivity (binding)
|
= -0.355
|
Selectivity of the compound (pC2-PC1) was determined
|
ChEMBL.
|
15177448
|