Activity (functional)
|
|
Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14
|
ChEMBL.
|
19351180
|
Activity (functional)
|
|
Antagonist activity at T7 epitope tagged human cloned sst2 expressed in HEK293 cells assessed as intracellular calcium release upto 10 uM
|
ChEMBL.
|
18543899
|
Activity (functional)
|
|
Agonist activity at T7-tagged human sst2 receptor expressed in HEK293 cells at 100 to 10000 nM
|
ChEMBL.
|
18410083
|
EC50 (functional)
|
= 0.18 nM
|
Concentration for inhibition of forskolin-stimulated cAMP accumulation in CCL39 cells
|
ChEMBL.
|
15658864
|
EC50 (functional)
|
= 0.77 nM
|
Concentration for inhibition of forskolin-stimulated cAMP accumulation in CCL39 cells
|
ChEMBL.
|
15658864
|
IC50 (functional)
|
nM
|
Antagonism of in vitro SRIF inhibition of GH release from rat pituitary cells in culture; not determined; not determined
|
ChEMBL.
|
11312929
|
IC50 (binding)
|
= 1.1 nM
|
Binding affinity to human sst3 by in vitro receptor autoradiography assay
|
ChEMBL.
|
24900340
|
IC50 (binding)
|
= 1.6 nM
|
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptor
|
ChEMBL.
|
18210999
|
IC50 (binding)
|
= 1.6 nM
|
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiography
|
ChEMBL.
|
20666484
|
IC50 (binding)
|
= 1.7 nM
|
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
|
ChEMBL.
|
19067538
|
IC50 (binding)
|
= 1.9 nM
|
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cells
|
ChEMBL.
|
19067538
|
IC50 (binding)
|
= 2 nM
|
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cells
|
ChEMBL.
|
19067538
|
IC50 (binding)
|
= 2 nM
|
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
|
ChEMBL.
|
19067538
|
IC50 (binding)
|
= 2 nM
|
Binding affinity to human sst1 by in vitro receptor autoradiography assay
|
ChEMBL.
|
24900340
|
IC50 (binding)
|
= 2.1 nM
|
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst5 receptor
|
ChEMBL.
|
18210999
|
IC50 (binding)
|
= 2.1 nM
|
Binding affinity to human sst5 by in vitro receptor autoradiography assay
|
ChEMBL.
|
24900340
|
IC50 (binding)
|
= 2.2 nM
|
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst1 receptor expressed in CHOK1 cells by autoradiography
|
ChEMBL.
|
18410083
|
IC50 (binding)
|
= 2.2 nM
|
Binding affinity to human sst4 by in vitro receptor autoradiography assay
|
ChEMBL.
|
24900340
|
IC50 (binding)
|
= 2.3 nM
|
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 2
|
ChEMBL.
|
15658864
|
IC50 (binding)
|
= 2.3 nM
|
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 2
|
ChEMBL.
|
15658864
|
IC50 (binding)
|
= 2.3 nM
|
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst1 receptor
|
ChEMBL.
|
18210999
|
IC50 (binding)
|
= 2.3 nM
|
Displacement of [125I]-[LTT] SIRF-28 from human SST1 receptor expressed in CHO cells by autoradiography
|
ChEMBL.
|
20666484
|
IC50 (binding)
|
= 2.4 nM
|
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 5
|
ChEMBL.
|
15658864
|
IC50 (binding)
|
= 2.4 nM
|
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 5
|
ChEMBL.
|
15658864
|
IC50 (binding)
|
= 2.4 nM
|
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst2 receptor expressed in chinese hamster CCL39 cells by autoradiography
|
ChEMBL.
|
18410083
|
IC50 (binding)
|
= 2.4 nM
|
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
|
ChEMBL.
|
18543899
|
IC50 (binding)
|
= 2.4 nM
|
Displacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiography
|
ChEMBL.
|
20666484
|
IC50 (binding)
|
= 2.4 nM
|
Binding affinity to human sst2 by in vitro receptor autoradiography assay
|
ChEMBL.
|
24900340
|
IC50 (binding)
|
= 2.5 nM
|
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst5 receptor expressed in CHOK1 cells by autoradiography
|
ChEMBL.
|
18410083
|
IC50 (binding)
|
= 2.6 nM
|
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
|
ChEMBL.
|
15658864
|
IC50 (binding)
|
= 2.6 nM
|
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
|
ChEMBL.
|
15658864
|
IC50 (binding)
|
= 2.6 nM
|
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cells
|
ChEMBL.
|
18410084
|
IC50 (binding)
|
= 2.6 nM
|
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
|
ChEMBL.
|
19067538
|
IC50 (binding)
|
= 2.6 nM
|
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
|
ChEMBL.
|
18543899
|
IC50 (binding)
|
= 2.6 nM
|
Displacement of [125I]LTT-SRIF-28 from human sst2 receptor by autoradiography
|
ChEMBL.
|
19351180
|
IC50 (binding)
|
= 2.7 nM
|
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst3 receptor expressed in chinese hamster CCL39 cells by autoradiography
|
ChEMBL.
|
18410083
|
IC50 (binding)
|
= 2.7 nM
|
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 cells by autoradiography
|
ChEMBL.
|
18410083
|
IC50 (binding)
|
= 2.7 nM
|
Displacement of [125I][LTT]SRIF28 from human cloned sst1 receptor by autoradiography
|
ChEMBL.
|
18543899
|
IC50 (binding)
|
= 2.7 nM
|
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiography
|
ChEMBL.
|
18543899
|
IC50 (binding)
|
= 2.9 nM
|
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiography
|
ChEMBL.
|
19351180
|
IC50 (binding)
|
= 2.9 nM
|
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
|
ChEMBL.
|
19351180
|
IC50 (binding)
|
= 2.9 nM
|
Displacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiography
|
ChEMBL.
|
19351180
|
IC50 (binding)
|
= 3 nM
|
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst2 receptor
|
ChEMBL.
|
18210999
|
IC50 (binding)
|
= 3 nM
|
Displacement of [125I]-[LTT] SIRF-28 from human SST2 receptor expressed in human CCL39 cells by autoradiography
|
ChEMBL.
|
20666484
|
IC50 (binding)
|
= 3.2 nM
|
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
|
ChEMBL.
|
15658864
|
IC50 (binding)
|
= 3.2 nM
|
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
|
ChEMBL.
|
15658864
|
IC50 (binding)
|
= 3.2 nM
|
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptor
|
ChEMBL.
|
18410084
|
IC50 (binding)
|
= 3.2 nM
|
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
|
ChEMBL.
|
18410084
|
IC50 (binding)
|
= 3.3 nM
|
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiography
|
ChEMBL.
|
18543899
|
IC50 (binding)
|
= 3.4 nM
|
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
|
ChEMBL.
|
18410084
|
IC50 (binding)
|
= 3.6 nM
|
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst3 receptor
|
ChEMBL.
|
18210999
|
IC50 (binding)
|
= 3.6 nM
|
Displacement of [125I]-[LTT] SIRF-28 from human SST3 receptor expressed in human CCL39 cells by autoradiography
|
ChEMBL.
|
20666484
|
IC50 (binding)
|
= 3.7 nM
|
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3
|
ChEMBL.
|
15658864
|
IC50 (binding)
|
= 3.7 nM
|
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3
|
ChEMBL.
|
15658864
|
IC50 (binding)
|
= 3.8 nM
|
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cells
|
ChEMBL.
|
18410084
|
IC50 (binding)
|
= 4.3 nM
|
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
|
ChEMBL.
|
19351180
|
Inhibition (binding)
|
= 0 %
|
Ability to displace [3H]-N-methylscopolamine binding to M1 human recombinant muscarinic receptor in CHO cells at concentration 1 microM.
|
ChEMBL.
|
10522693
|
Inhibition (binding)
|
= 0 %
|
Ability to displace [3H]-N-methylscopolamine binding to M2 human recombinant muscarinic receptor in CHO cells at concentration 1 microM.
|
ChEMBL.
|
10522693
|
Inhibition (binding)
|
= 2 %
|
Ability to displace [3H]-N-methylscopolamine binding to M1 human recombinant muscarinic receptor in CHO cells at concentration 10 microM.
|
ChEMBL.
|
10522693
|
Inhibition (binding)
|
= 8 %
|
Ability to displace [3H]-N-methylscopolamine binding to M2 human recombinant muscarinic receptor in CHO cells at concentration 10 microM
|
ChEMBL.
|
10522693
|
Inhibition (binding)
|
= 18 %
|
Ability to displace [3H]-N-methylscopolamine binding to M3 human recombinant muscarinic receptor in CHO cells at concentration 1 microM.
|
ChEMBL.
|
10522693
|
Inhibition (functional)
|
> 49 %
|
Inhibition of forskolin-stimulated cAMP accumulation in CCL39 cells
|
ChEMBL.
|
15658864
|
Inhibition (binding)
|
= 50 %
|
Ability to displace [3H]-N-methylscopolamine binding to M3 human recombinant muscarinic receptor in CHO cells at concentration 10 microM.
|
ChEMBL.
|
10522693
|
Inhibition (functional)
|
> 81 %
|
Inhibition of forskolin-stimulated cAMP accumulation in CCL39 cells
|
ChEMBL.
|
15658864
|
Ki (binding)
|
= 0.31 nM
|
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cells
|
ChEMBL.
|
11312929
|
Ki (binding)
|
= 0.4 nM
|
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
|
ChEMBL.
|
11312929
|
Ki (binding)
|
= 1.3 nM
|
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cells
|
ChEMBL.
|
11312929
|
Ki (binding)
|
= 1.9 nM
|
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cells
|
ChEMBL.
|
11312929
|
Ki (binding)
|
= 5.4 nM
|
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
|
ChEMBL.
|
11312929
|