Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
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name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
168288485 198510 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 430 8 2 4 5.0 Clc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5197201 198510 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 430 8 2 4 5.0 Clc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471936 198274 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 482 8 2 4 5.5 Fc1ccc2c(Cc3nnc(Cc4cccc(C(F)(F)F)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5193727 198274 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 482 8 2 4 5.5 Fc1ccc2c(Cc3nnc(Cc4cccc(C(F)(F)F)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
168296886 199286 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 5 4.4 COc1ccccc1Cc1nnc(Cc2c[nH]c3cc(F)ccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5209180 199286 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 5 4.4 COc1ccccc1Cc1nnc(Cc2c[nH]c3cc(F)ccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
168272821 197373 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 464 8 2 4 5.6 Clc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl 10.1039/D1MD00044F
CHEMBL5180543 197373 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 464 8 2 4 5.6 Clc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl 10.1039/D1MD00044F
142471848 198046 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 8 2 4 5.2 Fc1ccc2c(Cc3nnc(Cc4cccc(Br)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5190457 198046 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 8 2 4 5.2 Fc1ccc2c(Cc3nnc(Cc4cccc(Br)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
86293506 125597 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assayAgonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay
ChEMBL 309 3 2 3 2.4 Cc1cc2ccccc2c(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)n1 10.1021/ml500538a
CHEMBL3421842 125597 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assayAgonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay
ChEMBL 309 3 2 3 2.4 Cc1cc2ccccc2c(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)n1 10.1021/ml500538a
86294248 125598 1 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assayAgonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay
ChEMBL 298 3 2 4 1.4 Cn1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc21 10.1021/ml500538a
CHEMBL3421843 125598 1 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assayAgonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay
ChEMBL 298 3 2 4 1.4 Cn1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc21 10.1021/ml500538a
168280914 197581 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 426 9 2 5 4.3 COc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5183772 197581 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 426 9 2 5 4.3 COc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471730 197164 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 464 8 2 4 5.3 FC(F)(F)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5177487 197164 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 464 8 2 4 5.3 FC(F)(F)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471832 197054 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 471 8 3 4 5.1 Fc1ccc2c(Cc3nnc(Cc4c[nH]c5cc(F)ccc45)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5175637 197054 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 471 8 3 4 5.1 Fc1ccc2c(Cc3nnc(Cc4c[nH]c5cc(F)ccc45)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
168279197 197711 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 5 4.4 COc1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5185547 197711 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 5 4.4 COc1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
168272497 197012 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 448 8 2 4 5.1 Fc1ccc2c(Cc3nnc(Cc4cccc(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5174969 197012 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 448 8 2 4 5.1 Fc1ccc2c(Cc3nnc(Cc4cccc(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
168275406 197086 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 482 8 2 4 5.7 Fc1ccc2c(Cc3nnc(Cc4ccc(Cl)c(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5176083 197086 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 482 8 2 4 5.7 Fc1ccc2c(Cc3nnc(Cc4ccc(Cl)c(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
142471801 199078 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 494 9 2 5 5.3 COc1ccc2[nH]cc(Cc3nnc(Cc4cccc(C(F)(F)F)c4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
CHEMBL5206148 199078 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 494 9 2 5 5.3 COc1ccc2[nH]cc(Cc3nnc(Cc4cccc(C(F)(F)F)c4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
86292350 125599 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assayAgonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay
ChEMBL 303 3 2 4 1.8 CC(C)(NC(=O)[C@@H]1[C@H]2CNC[C@H]21)c1noc2c(F)cccc12 10.1021/ml500538a
CHEMBL3421844 125599 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assayAgonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay
ChEMBL 303 3 2 4 1.8 CC(C)(NC(=O)[C@@H]1[C@H]2CNC[C@H]21)c1noc2c(F)cccc12 10.1021/ml500538a
142471891 197374 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 430 8 2 4 5.0 Clc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5180551 197374 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 430 8 2 4 5.0 Clc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
168279055 198019 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 464 8 2 4 5.6 Clc1cc(Cl)cc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5190056 198019 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 464 8 2 4 5.6 Clc1cc(Cl)cc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471929 197946 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 414 8 2 4 4.4 Fc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5188841 197946 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 414 8 2 4 4.4 Fc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
168271257 197293 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 426 9 2 5 4.3 COc1ccccc1Cc1nnc(Cc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5179456 197293 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 426 9 2 5 4.3 COc1ccccc1Cc1nnc(Cc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
142471719 197281 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 9 1 5 5.5 Cn1cc(CCc2nnc(Cc3cccc(C(F)(F)F)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
CHEMBL5179321 197281 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 9 1 5 5.5 Cn1cc(CCc2nnc(Cc3cccc(C(F)(F)F)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
168271446 197384 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 421 8 2 5 4.2 N#Cc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5180752 197384 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 421 8 2 5 4.2 N#Cc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
168286554 198182 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 324 6 2 4 2.8 Fc1ccc2c(Cc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5192578 198182 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 324 6 2 4 2.8 Fc1ccc2c(Cc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
168283125 197856 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 441 9 2 4 5.2 NCCCCn1c(CCc2c[nH]c3ccccc23)nnc1Cc1ccc(Cl)c(Cl)c1 10.1039/D1MD00044F
CHEMBL5187484 197856 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 441 9 2 4 5.2 NCCCCn1c(CCc2c[nH]c3ccccc23)nnc1Cc1ccc(Cl)c(Cl)c1 10.1039/D1MD00044F
142471692 199161 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 440 10 2 5 4.5 COc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5207543 199161 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 440 10 2 5 4.5 COc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471938 198787 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 410 9 2 4 4.5 c1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5201594 198787 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 410 9 2 4 4.5 c1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
168295000 199251 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 474 9 2 6 3.7 CS(=O)(=O)c1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5208764 199251 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 474 9 2 6 3.7 CS(=O)(=O)c1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471828 198851 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 478 9 2 4 5.8 Clc1cc(Cl)cc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5202717 198851 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 478 9 2 4 5.8 Clc1cc(Cl)cc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471846 198108 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 4 5.1 Clc1ccccc1Cc1nnc(CCc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5191532 198108 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 4 5.1 Clc1ccccc1Cc1nnc(CCc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
142471682 198293 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 4 5.1 Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5193951 198293 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 4 5.1 Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471978 199222 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 396 8 2 4 4.3 c1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5208396 199222 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 396 8 2 4 4.3 c1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
168275268 196937 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 482 8 2 4 5.7 Fc1ccc2c(Cc3nnc(Cc4cc(Cl)cc(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5173784 196937 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 482 8 2 4 5.7 Fc1ccc2c(Cc3nnc(Cc4cc(Cl)cc(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
168274800 196871 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 9 2 6 3.8 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5172814 196871 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 9 2 6 3.8 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471665 198486 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 414 8 2 4 4.4 Fc1ccc2c(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5196971 198486 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 414 8 2 4 4.4 Fc1ccc2c(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
142471860 199284 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 428 9 2 4 4.6 Fc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5209165 199284 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 428 9 2 4 4.6 Fc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471737 197083 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 9 1 5 5.8 Cn1cc(CCc2nnc(Cc3ccc(Cl)c(Cl)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
CHEMBL5176020 197083 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 9 1 5 5.8 Cn1cc(CCc2nnc(Cc3ccc(Cl)c(Cl)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
142471923 198690 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 488 10 2 6 3.9 CS(=O)(=O)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5200112 198690 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 488 10 2 6 3.9 CS(=O)(=O)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471893 197106 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 516 12 2 5 6.1 c1ccc(COc2cccc(Cc3nnc(CCc4c[nH]c5ccccc45)n3CCCc3c[nH]cn3)c2)cc1 10.1039/D1MD00044F
CHEMBL5176454 197106 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 516 12 2 5 6.1 c1ccc(COc2cccc(Cc3nnc(CCc4c[nH]c5ccccc45)n3CCCc3c[nH]cn3)c2)cc1 10.1039/D1MD00044F
9893924 11520 34 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHOK1 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 2.5 to 20 hrs by TR-FRET assayAgonist activity at recombinant human SST4 receptor expressed in CHOK1 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 2.5 to 20 hrs by TR-FRET assay
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1039/C8MD00388B
CHEMBL103769 11520 34 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHOK1 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 2.5 to 20 hrs by TR-FRET assayAgonist activity at recombinant human SST4 receptor expressed in CHOK1 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 2.5 to 20 hrs by TR-FRET assay
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1039/C8MD00388B
142471814 198941 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 440 10 2 5 4.5 COc1ccccc1Cc1nnc(CCc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5203972 198941 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 440 10 2 5 4.5 COc1ccccc1Cc1nnc(CCc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
168296234 199067 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 430 8 2 4 5.0 Clc1ccccc1Cc1nnc(Cc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5205998 199067 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 430 8 2 4 5.0 Clc1ccccc1Cc1nnc(Cc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
142471924 197173 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 432 8 2 4 4.6 Fc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5177573 197173 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 432 8 2 4 4.6 Fc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471678 196821 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 474 9 2 6 3.7 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5171935 196821 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 474 9 2 6 3.7 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
139392666 196981 0 None -16 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST4Agonist activity at human SST4
ChEMBL 430 3 2 5 4.3 Cc1ccc(F)c2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
CHEMBL5174433 196981 0 None -16 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST4Agonist activity at human SST4
ChEMBL 430 3 2 5 4.3 Cc1ccc(F)c2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
117711399 125600 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assayAgonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay
ChEMBL 310 3 2 4 1.8 Cc1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc2n1 10.1021/ml500538a
CHEMBL3421845 125600 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assayAgonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay
ChEMBL 310 3 2 4 1.8 Cc1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc2n1 10.1021/ml500538a
142471772 197957 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 488 9 2 4 5.3 Brc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5189042 197957 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 488 9 2 4 5.3 Brc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
168271928 196862 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 306 6 2 4 2.7 c1ccc2c(Cc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5172730 196862 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 306 6 2 4 2.7 c1ccc2c(Cc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
142471769 198564 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 456 10 2 6 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccc(OC)cc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5198142 198564 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 456 10 2 6 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccc(OC)cc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471961 198200 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 494 10 2 5 5.4 FC(F)(F)Oc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5192791 198200 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 494 10 2 5 5.4 FC(F)(F)Oc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471655 197204 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 426 9 2 5 4.3 COc1ccc2[nH]cc(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
CHEMBL5178013 197204 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 426 9 2 5 4.3 COc1ccc2[nH]cc(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
142471841 198364 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 5 4.4 COc1ccc2[nH]cc(Cc3nnc(Cc4ccc(F)cc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
CHEMBL5195145 198364 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 5 4.4 COc1ccc2[nH]cc(Cc3nnc(Cc4ccc(F)cc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
142471677 198728 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 478 9 2 4 5.5 FC(F)(F)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5200786 198728 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 478 9 2 4 5.5 FC(F)(F)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
139392804 198382 1 None -16 5 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST4Agonist activity at human SST4
ChEMBL 412 3 2 5 4.1 Cc1cccc2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
CHEMBL5195355 198382 1 None -16 5 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST4Agonist activity at human SST4
ChEMBL 412 3 2 5 4.1 Cc1cccc2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
142471716 198271 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 5 4.4 COc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5193686 198271 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 5 4.4 COc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
56945132 178199 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHOK1 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 2.5 to 20 hrs by TR-FRET assayAgonist activity at recombinant human SST4 receptor expressed in CHOK1 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 2.5 to 20 hrs by TR-FRET assay
ChEMBL 478 9 2 4 5.8 Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl 10.1039/C8MD00388B
CHEMBL4462793 178199 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHOK1 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 2.5 to 20 hrs by TR-FRET assayAgonist activity at recombinant human SST4 receptor expressed in CHOK1 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 2.5 to 20 hrs by TR-FRET assay
ChEMBL 478 9 2 4 5.8 Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl 10.1039/C8MD00388B
168283525 197866 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 439 8 2 5 4.3 N#Cc1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5187631 197866 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 439 8 2 5 4.3 N#Cc1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471684 198231 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 426 9 2 5 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5193172 198231 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 426 9 2 5 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471767 199061 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 4 5.1 Clc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5205904 199061 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 4 5.1 Clc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471768 198783 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 435 9 2 5 4.4 N#Cc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5201540 198783 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 435 9 2 5 4.4 N#Cc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471733 197344 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 394 7 2 4 4.4 CC(C)(C)Cc1nnc(Cc2c[nH]c3cc(F)ccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5180116 197344 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 394 7 2 4 4.4 CC(C)(C)Cc1nnc(Cc2c[nH]c3cc(F)ccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
142471896 197922 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 446 9 2 4 4.8 Fc1cc(F)cc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5188361 197922 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 446 9 2 4 4.8 Fc1cc(F)cc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
168297256 199190 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 9 2 6 3.8 CS(=O)(=O)c1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5208037 199190 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 9 2 6 3.8 CS(=O)(=O)c1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471703 198511 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 455 10 2 6 4.4 O=[N+]([O-])c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5197218 198511 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 455 10 2 6 4.4 O=[N+]([O-])c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
43594 224481 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 542 9 4 12 -0.9 O[C@@H](C(=O)N[C@H]1[C@H]2SCC(CSC3=NN=NN3CS(O)(=O)=O)=C(N2C1=O)C(O)=O)C1=CC=CC=C1 None
38103 60566 69 None 6309 2 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 349 4 3 5 0.3 CC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)[C@H](N)C3=CCC=CC3)[C@H]2SC1 None
40467109 60566 69 None 6309 2 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 349 4 3 5 0.3 CC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)[C@H](N)C3=CCC=CC3)[C@H]2SC1 None
CHEMBL1604 60566 69 None 6309 2 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 349 4 3 5 0.3 CC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)[C@H](N)C3=CCC=CC3)[C@H]2SC1 None
6024 209488 79 None 7244 2 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 396 6 2 7 0.6 CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)Cc3cccs3)[C@H]2SC1 None
CHEMBL1632 209488 79 None 7244 2 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 396 6 2 7 0.6 CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)Cc3cccs3)[C@H]2SC1 None
CHEMBL617 209488 79 None 7244 2 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 396 6 2 7 0.6 CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)Cc3cccs3)[C@H]2SC1 None
30699 224483 0 None -1 14 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 423 7 2 8 0.5 CC(=O)OCC1=C(N2[C@H](SC1)[C@H](NC(=O)CSC1=CC=NC=C1)C2=O)C(O)=O None
7763 7198 0 None -380 2 Human 6.3 pIC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18543899
2027 7442 0 None -63 5 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11897676
2004 7429 0 None -19 2 Rat 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9166718
8487 10752 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11145612
9919857 10752 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11145612
DB12777 10752 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11145612
2079 8695 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14667212
2080 8696 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14667212
2012 8157 0 None -1 4 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15658864
2013 8961 0 None -2 6 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12450568
2026 7441 0 None -10 5 Human 6.5 pIC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11897676
2019 10447 0 None -79 4 Rat 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9166718
44386062 10447 0 None -79 4 Rat 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9166718
CHEMBL440072 10447 0 None -79 4 Rat 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9166718
2081 8697 0 None - 1 Human 8.5 pIC50 None 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14667212




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
124168080 188613 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at human SST4Agonist activity at human SST4
ChEMBL 507 6 2 7 4.4 Cc1cc(Cl)cc(-c2cnc3ncn(-c4cc(O)cc(F)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4778342 188613 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at human SST4Agonist activity at human SST4
ChEMBL 507 6 2 7 4.4 Cc1cc(Cl)cc(-c2cnc3ncn(-c4cc(O)cc(F)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
140762468 189462 0 None - 0 Human 6.0 pEC50 = 6 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 476 5 2 5 5.4 Cc1cc(C)cc(N2C=Nc3cc(Cl)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@H](C)N)c1 10.1021/acsmedchemlett.2c00431
CHEMBL4789268 189462 0 None - 0 Human 6.0 pEC50 = 6 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 476 5 2 5 5.4 Cc1cc(C)cc(N2C=Nc3cc(Cl)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@H](C)N)c1 10.1021/acsmedchemlett.2c00431
134168328 200318 0 None - 0 Human 6.0 pEC50 = 6 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 456 3 2 5 5.4 N#Cc1cccc(-c2ccc3ncc(-c4cc(F)cc(F)c4)c(N4CCC(N)CC4)c3c2)c1O 10.1021/acsmedchemlett.2c00431
CHEMBL4594359 200318 0 None - 0 Human 6.0 pEC50 = 6 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 456 3 2 5 5.4 N#Cc1cccc(-c2ccc3ncc(-c4cc(F)cc(F)c4)c(N4CCC(N)CC4)c3c2)c1O 10.1021/acsmedchemlett.2c00431
CHEMBL5267842 200318 0 None - 0 Human 6.0 pEC50 = 6 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 456 3 2 5 5.4 N#Cc1cccc(-c2ccc3ncc(-c4cc(F)cc(F)c4)c(N4CCC(N)CC4)c3c2)c1O 10.1021/acsmedchemlett.2c00431
nan 200318 0 None - 0 Human 6.0 pEC50 = 6 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 456 3 2 5 5.4 N#Cc1cccc(-c2ccc3ncc(-c4cc(F)cc(F)c4)c(N4CCC(N)CC4)c3c2)c1O 10.1021/acsmedchemlett.2c00431
CHEMBL5273084 200526 0 None - 0 Human 6.0 pEC50 = 6 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 438 3 2 5 5.2 N#Cc1cccc(-c2ccc3ncc(-c4cccc(F)c4)c(N4CCC(N)CC4)c3c2)c1O 10.1021/acsmedchemlett.2c00431
CHEMBL5283444 200988 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 431 3 2 4 5.5 NC1CCN(c2c(-c3cc(F)cc(F)c3)cnc3ccc(-c4cccc(O)c4)cc23)CC1 10.1021/acsmedchemlett.2c00431
124167759 187866 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 429 6 2 7 3.2 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CCN)c1 10.1021/acsmedchemlett.2c00431
CHEMBL4760001 187866 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 429 6 2 7 3.2 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CCN)c1 10.1021/acsmedchemlett.2c00431
124167759 187866 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 429 6 2 7 3.2 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CCN)c1 10.1021/acsmedchemlett.2c00431
CHEMBL4760001 187866 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 429 6 2 7 3.2 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CCN)c1 10.1021/acsmedchemlett.2c00431
CHEMBL5279994 200825 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 449 3 2 4 5.6 NC1CCN(c2c(-c3cc(F)cc(F)c3)cnc3ccc(-c4cccc(F)c4O)cc23)CC1 10.1021/acsmedchemlett.2c00431
140762567 187056 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at SST4 (unknown origin)Agonist activity at SST4 (unknown origin)
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(O)cc(F)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4750691 187056 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at SST4 (unknown origin)Agonist activity at SST4 (unknown origin)
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(O)cc(F)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL5271468 200464 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 390 7 4 5 4.1 Cc1cc(C)cc(-c2cncc(C(=O)Nc3cccc(O)c3)c2NCCCN)c1 10.1021/acsmedchemlett.2c00431
CHEMBL5271468 200464 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 390 7 4 5 4.1 Cc1cc(C)cc(-c2cncc(C(=O)Nc3cccc(O)c3)c2NCCCN)c1 10.1021/acsmedchemlett.2c00431
CHEMBL5279978 200824 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 411 5 3 4 4.6 Cc1cc(C)cc(-c2cncc(-c3ccc4c(O)cccc4c3)c2C(=O)NCCN)c1 10.1021/acsmedchemlett.2c00431
CHEMBL5279978 200824 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 411 5 3 4 4.6 Cc1cc(C)cc(-c2cncc(-c3ccc4c(O)cccc4c3)c2C(=O)NCCN)c1 10.1021/acsmedchemlett.2c00431
140762500 188512 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at SST4 (unknown origin)Agonist activity at SST4 (unknown origin)
ChEMBL 529 5 1 5 6.1 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)cc(C#N)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4777122 188512 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at SST4 (unknown origin)Agonist activity at SST4 (unknown origin)
ChEMBL 529 5 1 5 6.1 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)cc(C#N)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762573 189156 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at SST4 (unknown origin)Agonist activity at SST4 (unknown origin)
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(O)ccc4F)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4785112 189156 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at SST4 (unknown origin)Agonist activity at SST4 (unknown origin)
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(O)ccc4F)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
162648021 186752 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at SST4 (unknown origin)Agonist activity at SST4 (unknown origin)
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(F)c4O)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4746816 186752 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at SST4 (unknown origin)Agonist activity at SST4 (unknown origin)
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(F)c4O)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762468 189462 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 476 5 2 5 5.4 Cc1cc(C)cc(N2C=Nc3cc(Cl)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@H](C)N)c1 10.1021/acsmedchemlett.2c00431
CHEMBL4789268 189462 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 476 5 2 5 5.4 Cc1cc(C)cc(N2C=Nc3cc(Cl)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@H](C)N)c1 10.1021/acsmedchemlett.2c00431
16129706 215810 40 None -13 5 Human 10.1 pIC50 = 10.1 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR4Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR4
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm960850i
CHEMBL1823872 215810 40 None -13 5 Human 10.1 pIC50 = 10.1 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR4Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR4
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm960850i
CHEMBL262379 217317 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC1=O 10.1021/jm049520l
CHEMBL3350911 218308 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
CHEMBL415582 219969 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL2371100 216791 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm030246p
CHEMBL216992 216127 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049519m
CHEMBL406816 219402 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1824055 215818 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030246p
CHEMBL1824055 215818 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL1824055 215818 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm200307v
CHEMBL446380 220724 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL3350888 218290 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030246p
CHEMBL3350888 218290 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030245x
CHEMBL3350886 218288 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL3350908 218306 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](c1c[nH]c2ccccc12)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm030245x
CHEMBL3122129 217886 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysis
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)COCCOCCNC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2013.12.003
CHEMBL504087 220952 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CC(=O)N[C@@H]1CCSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL3350896 218297 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030246p
CHEMBL3350896 218297 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030245x
11468916 122241 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1137 15 14 14 0.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
CHEMBL3350910 122241 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1137 15 14 14 0.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
25188220 19263 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 11 4 4 4.2 C[C@H](NC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O)c1ccccc1 10.1021/jm801205x
CHEMBL1186489 19263 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 11 4 4 4.2 C[C@H](NC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O)c1ccccc1 10.1021/jm801205x
CHEMBL466609 19263 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 11 4 4 4.2 C[C@H](NC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O)c1ccccc1 10.1021/jm801205x
CHEMBL500326 220890 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL386784 219171 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049519m
11457521 122237 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1136 15 14 14 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL3350892 122237 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1136 15 14 14 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL3350884 218286 1 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030245x
CHEMBL3350905 218303 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
CHEMBL2371085 216790 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0302445
CHEMBL3350891 218293 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL3350893 218294 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL3350899 218300 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL3122128 217885 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysis
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)COCCOCCNC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2013.12.003
CHEMBL263587 217357 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049519m
CHEMBL3350898 218299 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL3350912 218309 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
25187400 19466 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 537 10 4 4 3.7 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1187495 19466 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 537 10 4 4 3.7 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL504930 19466 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 537 10 4 4 3.7 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL504457 220956 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL265912 217450 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 4.Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 4.
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm010037+
CHEMBL2371060 216786 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0302445
CHEMBL504248 220954 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CC(=O)N[C@H]1CCSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL410047 219576 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049519m
11389178 122238 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1136 15 14 14 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL3350900 122238 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1136 15 14 14 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL503036 220939 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CC(=O)N[C@@H]1CSS[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL3350895 218296 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL442494 220692 0 None -17 5 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm070886i
CHEMBL442494 220692 0 None -17 5 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiography
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm1005868
16129706 215810 40 None -13 5 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysis
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.ejmech.2013.12.003
CHEMBL1823872 215810 40 None -13 5 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysis
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.ejmech.2013.12.003
CHEMBL447989 220732 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CC(=O)N[C@@H]1SS[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
16129706 215810 40 None -13 5 Human 8.8 pIC50 = 8.8 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm049519m
CHEMBL1823872 215810 40 None -13 5 Human 8.8 pIC50 = 8.8 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm049519m
16129706 215810 40 None -13 5 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm200307v
CHEMBL1823872 215810 40 None -13 5 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm200307v
CHEMBL408338 219485 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm049520l
CHEMBL409100 219525 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 4.Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 4.
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@@H]1CSSC[C@H](C(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm010037+
16129706 215810 40 None -13 5 Human 8.8 pIC50 = 8.8 Binding
Inhibition of human SSTR4 by radioligand binding assayInhibition of human SSTR4 by radioligand binding assay
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.ejmech.2018.11.030
CHEMBL1823872 215810 40 None -13 5 Human 8.8 pIC50 = 8.8 Binding
Inhibition of human SSTR4 by radioligand binding assayInhibition of human SSTR4 by radioligand binding assay
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.ejmech.2018.11.030
CHEMBL406373 219385 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(I)cc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL425090 220108 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL452157 220755 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030246p
CHEMBL3350881 218283 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL3350897 218298 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](c1c[nH]c2ccccc12)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm030245x
CHEMBL452157 220755 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL452157 220755 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm200307v
CHEMBL452157 220755 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL452157 220755 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm801314f
CHEMBL452157 220755 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049519m
CHEMBL3350894 218295 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL505128 220967 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CC(=O)N[C@@H]1SSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
11563877 171499 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 668 9 3 5 5.7 Cc1cc(F)ccc1N1CCN(C(=O)N[C@@H](C(=O)Nc2cc(CN(C)C)ccc2OC(F)(F)F)[C@@H](C)c2c[nH]c3ccccc23)CC1=O 10.1016/j.bmc.2017.09.031
CHEMBL4217405 171499 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 668 9 3 5 5.7 Cc1cc(F)ccc1N1CCN(C(=O)N[C@@H](C(=O)Nc2cc(CN(C)C)ccc2OC(F)(F)F)[C@@H](C)c2c[nH]c3ccccc23)CC1=O 10.1016/j.bmc.2017.09.031
44298251 201450 0 None - 1 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration required against human Somatostatin receptor type 4Inhibitory concentration required against human Somatostatin receptor type 4
ChEMBL 668 20 3 8 6.1 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)C(OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm0205088
CHEMBL53204 201450 0 None - 1 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration required against human Somatostatin receptor type 4Inhibitory concentration required against human Somatostatin receptor type 4
ChEMBL 668 20 3 8 6.1 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)C(OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm0205088
56681776 70015 0 None - 0 Human 7.0 pIC50 = 7 Binding
Tested for binding affinity against human somatostatin receptor subtype 4 (hSSTR4)Tested for binding affinity against human somatostatin receptor subtype 4 (hSSTR4)
ChEMBL 802 9 7 8 2.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)C2C(=O)[C@@H](Cc3c2[nH]c2ccccc32)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCC2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm000316h
CHEMBL1790896 70015 0 None - 0 Human 7.0 pIC50 = 7 Binding
Tested for binding affinity against human somatostatin receptor subtype 4 (hSSTR4)Tested for binding affinity against human somatostatin receptor subtype 4 (hSSTR4)
ChEMBL 802 9 7 8 2.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)C2C(=O)[C@@H](Cc3c2[nH]c2ccccc32)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCC2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm000316h
118718507 122136 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL 1050 14 11 12 3.4 CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)NC(C)(C)C)NC1=O 10.1021/jm970730q
CHEMBL3349670 122136 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL 1050 14 11 12 3.4 CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)NC(C)(C)C)NC1=O 10.1021/jm970730q
CHEMBL2079558 215973 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL2079559 215974 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2cccc(-c3ccccc3)c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL2079563 215975 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm970730q
10796238 215976 2 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm970730q
CHEMBL2079626 215976 2 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm970730q
DB06791 215976 2 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm970730q
CHEMBL2311181 216286 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL3349505 218189 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/jm970730q
CHEMBL3349508 218192 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/jm970730q
CHEMBL3349597 218205 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/jm970730q
CHEMBL3349608 218215 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2cccnc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm970730q
CHEMBL3349610 218216 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(C)(C)SSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm970730q
CHEMBL3349611 218217 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm970730q
CHEMBL3349612 218218 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccccc2)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm970730q
CHEMBL3349613 218219 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccccc2)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm970730q
CHEMBL3349614 218220 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm970730q
CHEMBL3349617 218222 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2cccnc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm970730q
CHEMBL3349618 218223 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2cccnc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm970730q
CHEMBL3349663 218226 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2cccc(-c3ccccc3)c2)CSSC[C@@H](C(=O)N[C@@H](Cc2cccc(-c3ccccc3)c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL3349665 218228 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2cccc(-c3ccccc3)c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL3349666 218229 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2cccc(-c3ccccc3)c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL3349667 218230 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2cccc(-c3ccccc3)c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL3349671 218233 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(-c3ccccc3)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL3349672 218234 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL3349673 218235 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL3349674 218236 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/jm970730q
CHEMBL3349675 218237 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm970730q
CHEMBL3349676 218238 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccccc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL3349677 218239 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL3349679 218241 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm970730q
CHEMBL3349680 218242 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/jm970730q
CHEMBL3351090 218323 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
49865345 22683 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiography
ChEMBL 1043 18 13 12 0.7 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C/C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cc3ccccc3[nH]2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1 10.1021/jm1005868
CHEMBL1223230 22683 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiography
ChEMBL 1043 18 13 12 0.7 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C/C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cc3ccccc3[nH]2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1 10.1021/jm1005868
155526536 177978 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human SSTR4 by radioligand binding assayInhibition of human SSTR4 by radioligand binding assay
ChEMBL 1405 26 16 21 -3.2 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1016/j.ejmech.2018.11.030
CHEMBL4459308 177978 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human SSTR4 by radioligand binding assayInhibition of human SSTR4 by radioligand binding assay
ChEMBL 1405 26 16 21 -3.2 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1016/j.ejmech.2018.11.030
CHEMBL2372606 217055 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccccc2)NC[C@H]2O[C@H](O)[C@H](O)[C@@H](O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL2372608 217055 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccccc2)NC[C@H]2O[C@H](O)[C@H](O)[C@@H](O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
10577746 214031 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration required for somatostatin 4 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 4 receptor in radioligand binding assay ([125I]Tyr11-SRIF)
ChEMBL 514 8 3 4 4.6 NCCCC[C@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)SCCN(Cc2cccc3ccccc23)C1=O 10.1016/s0960-894x(00)00552-7
CHEMBL92914 214031 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration required for somatostatin 4 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 4 receptor in radioligand binding assay ([125I]Tyr11-SRIF)
ChEMBL 514 8 3 4 4.6 NCCCC[C@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)SCCN(Cc2cccc3ccccc23)C1=O 10.1016/s0960-894x(00)00552-7
CHEMBL414544 219919 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
162646037 186293 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR4 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR4 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1387 27 17 19 -2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4741230 186293 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR4 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR4 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1387 27 17 19 -2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL387458 219189 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL455435 220782 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 cells by autoradiography
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CCSSCC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm701445q
44560867 195919 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL 1204 18 12 14 1.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N(C)C(=O)c2ccccc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL510693 195919 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL 1204 18 12 14 1.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N(C)C(=O)c2ccccc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL3349598 218206 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm970730q
CHEMBL414446 219910 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@H](c1ccc2ccccc2c1)[C@@H]1NC(=O)[C@H](Cc2ccc(I)cc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL1824051 215814 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm200307v
CHEMBL1824052 215815 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm200307v
56651206 181410 0 None 1 2 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 659 11 5 9 3.8 NCCCCO[C@@H]1[C@@H](NC(=O)Cc2c[nH]c3ccccc23)COC(=O)c2c(O)cccc2CCCOC[C@@H](OCc2ccccc2)[C@H]1O 10.1016/j.ejmech.2018.11.030
CHEMBL4557933 181410 0 None 1 2 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 659 11 5 9 3.8 NCCCCO[C@@H]1[C@@H](NC(=O)Cc2c[nH]c3ccccc23)COC(=O)c2c(O)cccc2CCCOC[C@@H](OCc2ccccc2)[C@H]1O 10.1016/j.ejmech.2018.11.030
16737812 92281 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptor
ChEMBL 508 10 3 3 4.9 NCCCCCN1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm070246f
CHEMBL227211 92281 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptor
ChEMBL 508 10 3 3 4.9 NCCCCCN1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm070246f
118718854 122194 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350354 122194 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350902 218302 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N(C)[C@H](C(=O)c2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030246p
CHEMBL509192 222113 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(N)=O)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
44368019 17037 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1136 12 12 15 1.1 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)N(C(=O)c2ccccc2)C(=O)N(C)[C@H](O)NC(=O)[C@@H](N)CSSCCNC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1161328 17037 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1136 12 12 15 1.1 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)N(C(=O)c2ccccc2)C(=O)N(C)[C@H](O)NC(=O)[C@@H](N)CSSCCNC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
25187683 19223 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 627 12 4 4 5.2 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1186082 19223 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 627 12 4 4 5.2 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL448713 19223 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 627 12 4 4 5.2 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C1=O 10.1021/jm801205x
25188218 19336 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 11 4 4 4.2 C[C@@H](NC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O)c1ccccc1 10.1021/jm801205x
CHEMBL1186753 19336 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 11 4 4 4.2 C[C@@H](NC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O)c1ccccc1 10.1021/jm801205x
CHEMBL476240 19336 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 11 4 4 4.2 C[C@@H](NC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O)c1ccccc1 10.1021/jm801205x
24777672 101687 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptor
ChEMBL 1027 18 12 11 1.0 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1 10.1021/jm070886i
CHEMBL254210 101687 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptor
ChEMBL 1027 18 12 11 1.0 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1 10.1021/jm070886i
118718854 122194 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350354 122194 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350901 218301 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)N(C)[C@H](C(=O)c2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030246p
44368398 17038 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1196 16 15 16 -0.2 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1161331 17038 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1196 16 15 16 -0.2 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1824050 215813 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm200307v
25187681 19241 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 613 11 4 4 5.3 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccc(-c3ccccc3)cc2)C1=O 10.1021/jm801205x
CHEMBL1186190 19241 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 613 11 4 4 5.3 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccc(-c3ccccc3)cc2)C1=O 10.1021/jm801205x
CHEMBL453412 19241 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 613 11 4 4 5.3 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccc(-c3ccccc3)cc2)C1=O 10.1021/jm801205x
25189327 19468 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 601 11 4 4 4.7 NCCCC[C@@H](C(=O)NCc1cccc2ccccc12)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1187509 19468 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 601 11 4 4 4.7 NCCCC[C@@H](C(=O)NCc1cccc2ccccc12)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL505888 19468 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 601 11 4 4 4.7 NCCCC[C@@H](C(=O)NCc1cccc2ccccc12)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL455760 220787 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 cells by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2c[nH]c(C(=O)O)c2)CCSSCC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701445q
44368398 17038 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1196 16 15 16 -0.2 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1161331 17038 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1196 16 15 16 -0.2 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
46919128 23858 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 552 12 4 7 2.5 CS[C@@H]1O[C@H](COCc2ccccc2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCN=C(N)N 10.1021/jm1002777
CHEMBL1254882 23858 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 552 12 4 7 2.5 CS[C@@H]1O[C@H](COCc2ccccc2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCN=C(N)N 10.1021/jm1002777
CHEMBL3350909 218307 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030245x
CHEMBL442494 220692 0 None -17 5 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm801205x
CHEMBL504395 220955 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CC(=O)N[C@H]1CSS[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL2111200 215994 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL3350890 218292 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
25187953 19461 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 725 10 4 6 3.8 CS(=O)(=O)N1CC2(CCN(C(=O)N[C@@H]3Cc4c([nH]c5ccccc45)CN([C@@H](CCCCN)C(=O)NCc4ccccc4)C3=O)CC2)c2ccccc21 10.1021/jm801205x
CHEMBL1187458 19461 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 725 10 4 6 3.8 CS(=O)(=O)N1CC2(CCN(C(=O)N[C@@H]3Cc4c([nH]c5ccccc45)CN([C@@H](CCCCN)C(=O)NCc4ccccc4)C3=O)CC2)c2ccccc21 10.1021/jm801205x
CHEMBL503379 19461 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 725 10 4 6 3.8 CS(=O)(=O)N1CC2(CCN(C(=O)N[C@@H]3Cc4c([nH]c5ccccc45)CN([C@@H](CCCCN)C(=O)NCc4ccccc4)C3=O)CC2)c2ccccc21 10.1021/jm801205x
CHEMBL2111257 215995 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@H](C)c2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0302445
CHEMBL442494 220692 0 None -17 5 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human sst4 by in vitro receptor autoradiography assayBinding affinity to human sst4 by in vitro receptor autoradiography assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/ml200032v
CHEMBL506892 220995 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CC(=O)N[C@H]1SS[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL3350357 218254 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm030246p
118719101 122218 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1356 21 16 16 2.5 CNc1ccc(C(C(C)C)[C@@H]2NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC2=O)cc1 10.1021/jm030245x
CHEMBL3350724 122218 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1356 21 16 16 2.5 CNc1ccc(C(C(C)C)[C@@H]2NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC2=O)cc1 10.1021/jm030245x
CHEMBL2371059 216785 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None CNc1ccc(C(C(C)C)[C@@H]2NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC2=O)cc1 10.1021/jm030245x
CHEMBL1823873 215811 9 None -18 4 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm200307v
25187679 19443 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 571 10 4 4 4.3 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccc(Cl)cc2)C1=O 10.1021/jm801205x
CHEMBL1187340 19443 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 571 10 4 4 4.3 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccc(Cl)cc2)C1=O 10.1021/jm801205x
CHEMBL499398 19443 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 571 10 4 4 4.3 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccc(Cl)cc2)C1=O 10.1021/jm801205x
CHEMBL3350880 218282 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None CNc1ccc(C[C@@H]2NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC2=O)cc1 10.1021/jm030245x
CHEMBL3350882 218284 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030245x
25189325 19218 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 12 4 4 3.6 NCCCC[C@@H](C(=O)NCCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1186056 19218 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 12 4 4 3.6 NCCCC[C@@H](C(=O)NCCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL447455 19218 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 12 4 4 3.6 NCCCC[C@@H](C(=O)NCCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
25188496 19307 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 476 9 3 5 2.5 COC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1186630 19307 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 476 9 3 5 2.5 COC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL473160 19307 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 476 9 3 5 2.5 COC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1907758 215847 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm030245x
CHEMBL3350889 218291 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None CNc1ccc(C[C@@H]2NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC2=O)cc1 10.1021/jm030245x
CHEMBL501776 220923 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL524870 222404 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CC(=O)N[C@@H]1SS[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL442494 220692 0 None -17 5 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm701618q
CHEMBL442494 220692 0 None -17 5 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm049520l
CHEMBL505496 220972 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CC(=O)N[C@H]1SS[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL442494 220692 0 None -17 5 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 cells by autoradiography
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm701445q
CHEMBL2111200 215994 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm030246p
CHEMBL3122127 217884 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysis
ChEMBL None None None C[C@H](NC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)C(=O)NCC(=O)N[C@H]1CSSC[C@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1016/j.ejmech.2013.12.003
CHEMBL442494 220692 0 None -17 5 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm801314f
CHEMBL407649 219453 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccc(I)cc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
155550820 181068 0 None -5 2 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 1275 22 16 18 -2.3 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)C(C)C)NC(=O)[C@H](CC(=O)N[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2NC(C)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2018.11.030
CHEMBL4549840 181068 0 None -5 2 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 1275 22 16 18 -2.3 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)C(C)C)NC(=O)[C@H](CC(=O)N[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2NC(C)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2018.11.030
11535351 103827 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptor
ChEMBL 983 17 13 12 -0.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)CCCC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm070886i
CHEMBL267054 103827 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptor
ChEMBL 983 17 13 12 -0.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)CCCC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm070886i
CHEMBL526550 222471 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 cells by autoradiography
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccccc2)SS1)C(N)=O 10.1021/jm701445q
70683416 80742 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1170 16 9 12 4.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL2021544 80742 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1170 16 9 12 4.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
44388037 167758 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1659 18 18 20 0.0 CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3I)C(=O)N[C@@H]3CCCCCCNC(=O)CC[C@@H](NC(=O)[C@@H](Cc4ccccc4)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC3=O)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049519m
CHEMBL411600 167758 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1659 18 18 20 0.0 CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3I)C(=O)N[C@@H]3CCCCCCNC(=O)CC[C@@H](NC(=O)[C@@H](Cc4ccccc4)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC3=O)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049519m
155553012 180865 0 None 1 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 511 10 5 7 2.3 Cc1ccc(S[C@H]2O[C@H](CO)[C@@H](O)[C@H](OC/C=C/CN)[C@@H]2NC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.ejmech.2018.11.030
CHEMBL4544582 180865 0 None 1 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 511 10 5 7 2.3 Cc1ccc(S[C@H]2O[C@H](CO)[C@@H](O)[C@H](OC/C=C/CN)[C@@H]2NC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.ejmech.2018.11.030
155541897 179834 0 None -5 2 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 583 7 3 9 3.7 CC(C)CCO[C@@H]1[C@@H](O)[C@@H](O)[C@H]2Cn3cc(nn3)COCCCCCCN(CCc3c[nH]c4ccccc34)CC[C@H]1O2 10.1016/j.ejmech.2018.11.030
CHEMBL4519358 179834 0 None -5 2 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 583 7 3 9 3.7 CC(C)CCO[C@@H]1[C@@H](O)[C@@H](O)[C@H]2Cn3cc(nn3)COCCCCCCN(CCc3c[nH]c4ccccc34)CC[C@H]1O2 10.1016/j.ejmech.2018.11.030
CHEMBL425465 220114 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)O)CSSC[C@@H](N)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049520l
CHEMBL367125 218937 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049519m
44368398 17038 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1196 16 15 16 -0.2 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1161331 17038 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1196 16 15 16 -0.2 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL414692 219926 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)O)CSSC[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049520l
49865344 22682 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiography
ChEMBL 1031 17 13 12 0.3 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C/C=C\C[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm1005868
CHEMBL1223229 22682 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiography
ChEMBL 1031 17 13 12 0.3 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C/C=C\C[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm1005868
CHEMBL1824049 215812 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm200307v
CHEMBL540408 222493 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL554624 222505 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](N)Cc3ccccc3)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
42637563 202289 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 989 12 9 12 2.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc3ccc(O)cc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL553656 202289 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 989 12 9 12 2.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc3ccc(O)cc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL265846 217446 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 4.Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 4.
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(CN)cc2)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC1=O 10.1021/jm010037+
42637503 202596 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1238 19 12 15 2.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL558161 202596 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1238 19 12 15 2.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
42637632 67049 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1334 20 11 14 5.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL174206 67049 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1334 20 11 14 5.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL3349506 218190 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/jm970730q
CHEMBL448431 220736 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL508585 221773 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)CSSC[C@@H](C(=O)N[C@H](Cc2ccc(O)cc2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL452074 220753 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 cells by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2c[nH]c(C(=O)O)c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701445q
45273129 202516 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1173 19 14 15 1.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(C(N)=O)cc2)CSS[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)O)NC1=O 10.1021/jm801314f
CHEMBL557288 202516 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1173 19 14 15 1.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(C(N)=O)cc2)CSS[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)O)NC1=O 10.1021/jm801314f
CHEMBL510755 222367 0 None - 3 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
11159133 122240 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1152 15 15 15 0.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
CHEMBL3350904 122240 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1152 15 15 15 0.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
CHEMBL453936 220769 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CC(=O)N[C@@H]1CSS[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL1907758 215847 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=5)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=5)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm040794i
13690207 122160 0 None -2041 5 Human 8.5 pIC50 = 8.5 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR4Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR4
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm960850i
CHEMBL3350037 122160 0 None -2041 5 Human 8.5 pIC50 = 8.5 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR4Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR4
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm960850i
CHEMBL1907758 215847 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL525030 222410 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CC(=O)N[C@H]1SSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL3350887 218289 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None CNc1ccc(C[C@@H]2NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC2=O)cc1 10.1021/jm030245x
CHEMBL505854 220977 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CC(=O)N[C@@H]1CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
16737814 92282 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL227212 92282 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL504838 92282 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
16737814 92282 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptor
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
CHEMBL227212 92282 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptor
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
CHEMBL504838 92282 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptor
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
CHEMBL436962 220479 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC1=O 10.1021/jm049519m
16737814 92282 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human SSTR4 by radioligand binding assayInhibition of human SSTR4 by radioligand binding assay
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1016/j.ejmech.2018.11.030
CHEMBL227212 92282 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human SSTR4 by radioligand binding assayInhibition of human SSTR4 by radioligand binding assay
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1016/j.ejmech.2018.11.030
CHEMBL504838 92282 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human SSTR4 by radioligand binding assayInhibition of human SSTR4 by radioligand binding assay
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1016/j.ejmech.2018.11.030
118718854 122194 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350354 122194 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL442494 220692 0 None -17 5 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm701444y
CHEMBL3350357 218254 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL2371108 216792 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm030246p
CHEMBL3350913 218310 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030246p
CHEMBL3350725 218269 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)c(I)c2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030245x
CHEMBL2369533 216411 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 4.Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 4.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](CO)NC1=O 10.1021/jm010037+
CHEMBL3122130 217887 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysis
ChEMBL None None None C[C@H](NC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.ejmech.2013.12.003
CHEMBL1907758 215847 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm030243c
CHEMBL410184 219585 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@H](c1ccc2ccccc2c1)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(I)cc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL262135 217306 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL None None None None 10.1021/jm040794i
CHEMBL3349668 218231 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2cccc(-c3ccccc3)c2)CSSC[C@@H](C(=O)N[C@@H](Cc2cccc(-c3ccccc3)c2)C(N)=O)NC1=O 10.1021/jm970730q
118718854 122194 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350354 122194 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL2079558 215973 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
122179457 128232 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to somatostatin receptor type 4 (unknown origin)Binding affinity to somatostatin receptor type 4 (unknown origin)
ChEMBL 495 4 3 8 3.7 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL3582317 128232 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to somatostatin receptor type 4 (unknown origin)Binding affinity to somatostatin receptor type 4 (unknown origin)
ChEMBL 495 4 3 8 3.7 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL1908984 215851 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](N)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC2=O)cc1 10.1021/jm801314f
CHEMBL563124 215851 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](N)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC2=O)cc1 10.1021/jm801314f
CHEMBL2372604 217054 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL None None None C[C@H](O)[C@@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
CHEMBL2372607 217054 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL None None None C[C@H](O)[C@@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
49865343 22681 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiography
ChEMBL 1147 20 12 13 2.2 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cc3ccccc3[nH]2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(OC(=O)c3ccccc3)cc2)C(=O)N1 10.1021/jm1005868
CHEMBL1223228 22681 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiography
ChEMBL 1147 20 12 13 2.2 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cc3ccccc3[nH]2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(OC(=O)c3ccccc3)cc2)C(=O)N1 10.1021/jm1005868
CHEMBL2372603 217053 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=2)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=2)
ChEMBL None None None C[C@H](O)[C@@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
CHEMBL447064 220726 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL None None None CC(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm701618q
25187955 19208 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 646 9 4 4 4.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCC3(CCc4ccccc43)CC2)C1=O 10.1021/jm801205x
CHEMBL1185951 19208 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 646 9 4 4 4.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCC3(CCc4ccccc43)CC2)C1=O 10.1021/jm801205x
CHEMBL443084 19208 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 646 9 4 4 4.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCC3(CCc4ccccc43)CC2)C1=O 10.1021/jm801205x
CHEMBL2372667 217059 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity of human Somatostatin receptor type 4 (hsst4) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 4 (hsst4) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(NC(=O)[C@@H](N)Cc2ccccc2)CSSCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
90663875 113518 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL 1424 23 18 21 -2.3 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CCS[C@@H]2O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3144287 113518 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL 1424 23 18 21 -2.3 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CCS[C@@H]2O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL5282589 200943 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human somatostatin receptor type 4Inhibition of human somatostatin receptor type 4
ChEMBL 633 14 7 7 0.1 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C1=O 10.1021/acs.jmedchem.6b01029
CHEMBL2011466 215893 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human sst4 by in vitro receptor autoradiography assayBinding affinity to human sst4 by in vitro receptor autoradiography assay
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)N(C)C(=O)[C@H](Cc2ccccc2)N(C)C1=O 10.1021/ml200032v
44368406 17039 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1022 9 11 12 1.1 C[C@@H]1NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1161332 17039 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1022 9 11 12 1.1 C[C@@H]1NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
10114 9334 23 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]SS-28 from human SSTR-4 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR-4 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Fc1ccc(cc1)c1cnc([nH]1)[C@H]1Cc2c3ccccc3[nH]c2[C@@](N1)(c1noc(n1)C)c1cnn(c1)C 10.1021/ml300063m
56927659 9334 23 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]SS-28 from human SSTR-4 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR-4 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Fc1ccc(cc1)c1cnc([nH]1)[C@H]1Cc2c3ccccc3[nH]c2[C@@](N1)(c1noc(n1)C)c1cnn(c1)C 10.1021/ml300063m
CHEMBL2204935 9334 23 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]SS-28 from human SSTR-4 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR-4 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Fc1ccc(cc1)c1cnc([nH]1)[C@H]1Cc2c3ccccc3[nH]c2[C@@](N1)(c1noc(n1)C)c1cnn(c1)C 10.1021/ml300063m
CHEMBL436887 220470 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL3350885 218287 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H]([C@H](C)c2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL3122123 217881 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysis
ChEMBL None None None CCCC[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2013.12.003
CHEMBL2372713 217063 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity of human Somatostatin receptor type 4 (hsst4) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 4 (hsst4) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
2082 9039 14 None 7079 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1021/jm0302445
5311374 9039 14 None 7079 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1021/jm0302445
CHEMBL1450103 9039 14 None 7079 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1021/jm0302445
2082 9039 14 None 7079 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1021/jm030243c
5311374 9039 14 None 7079 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1021/jm030243c
CHEMBL1450103 9039 14 None 7079 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1021/jm030243c
2082 9039 14 None 7079 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1021/jm030245x
5311374 9039 14 None 7079 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1021/jm030245x
CHEMBL1450103 9039 14 None 7079 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1021/jm030245x
11343811 122239 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1152 15 15 15 0.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
CHEMBL3350903 122239 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1152 15 15 15 0.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
25189052 19444 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 676 10 5 6 3.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C1=O 10.1021/jm801205x
CHEMBL1187345 19444 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 676 10 5 6 3.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C1=O 10.1021/jm801205x
CHEMBL499681 19444 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 676 10 5 6 3.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C1=O 10.1021/jm801205x
CHEMBL504462 220958 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CC(=O)N[C@@H]1SSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL503596 220949 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
46902023 23810 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 544 11 3 7 3.7 COC[C@H]1O[C@@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCN)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254476 23810 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 544 11 3 7 3.7 COC[C@H]1O[C@@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCN)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL3349616 218221 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm970730q
CHEMBL2371051 216783 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0302445
CHEMBL1824056 215819 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm200307v
44325273 214087 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration required for somatostatin 4 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 4 receptor in radioligand binding assay ([125I]Tyr11-SRIF)
ChEMBL 554 7 2 4 5.4 NCCCC1CCCN2C(=O)[C@@H](Cc3c[nH]c4ccccc34)SCCN(Cc3cccc4ccccc34)C(=O)C12 10.1016/s0960-894x(00)00552-7
CHEMBL93351 214087 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration required for somatostatin 4 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 4 receptor in radioligand binding assay ([125I]Tyr11-SRIF)
ChEMBL 554 7 2 4 5.4 NCCCC1CCCN2C(=O)[C@@H](Cc3c[nH]c4ccccc34)SCCN(Cc3cccc4ccccc34)C(=O)C12 10.1016/s0960-894x(00)00552-7
44444935 101417 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptor
ChEMBL 981 17 13 12 -0.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C/C=C\C[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm070886i
CHEMBL252355 101417 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptor
ChEMBL 981 17 13 12 -0.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C/C=C\C[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm070886i
49865341 22679 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiography
ChEMBL 981 17 13 12 -0.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C/C=C\C[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm1005868
CHEMBL1223226 22679 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiography
ChEMBL 981 17 13 12 -0.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C/C=C\C[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm1005868
CHEMBL437905 220517 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)N(C)C(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL262790 217330 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(N)=O)CSSC[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049520l
44368422 17040 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1123 10 13 14 -0.0 C[C@H]1C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(=O)O)CSSC[C@@H](N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](O)NC(=O)N1C 10.1021/jm030243c
CHEMBL1161333 17040 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1123 10 13 14 -0.0 C[C@H]1C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(=O)O)CSSC[C@@H](N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](O)NC(=O)N1C 10.1021/jm030243c
11642413 23872 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 544 11 3 7 3.9 CS[C@@H]1O[C@H](COCc2ccc(Cl)cc2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCN 10.1021/jm1002777
CHEMBL1254967 23872 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 544 11 3 7 3.9 CS[C@@H]1O[C@H](COCc2ccc(Cl)cc2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCN 10.1021/jm1002777
44388123 175965 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1681 21 18 21 0.2 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3I)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL440618 175965 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1681 21 18 21 0.2 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3I)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
11548587 23887 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 560 11 3 7 4.4 CS[C@@H]1O[C@H](COCc2ccc3ccccc3c2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCN 10.1021/jm1002777
CHEMBL1255049 23887 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 560 11 3 7 4.4 CS[C@@H]1O[C@H](COCc2ccc3ccccc3c2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCN 10.1021/jm1002777
45268875 202389 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1363 19 12 15 2.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3I)CSSC[C@@H](C(=O)N[C@@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL555977 202389 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1363 19 12 15 2.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3I)CSSC[C@@H](C(=O)N[C@@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL441920 220679 13 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL499939 220883 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)c(I)c2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)CSSC[C@@H](C(=O)N[C@H](Cc2ccc(O)cc2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL1908982 215850 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC2=O)cc1 10.1021/jm801314f
CHEMBL552988 215850 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC2=O)cc1 10.1021/jm801314f
CHEMBL502219 220930 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
90663869 113514 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL 1424 23 18 21 -2.3 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CCS[C@@H]2O[C@@H](CO)[C@H](O)[C@H](O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3144281 113514 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL 1424 23 18 21 -2.3 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CCS[C@@H]2O[C@@H](CO)[C@H](O)[C@H](O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL413441 219850 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 4.Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 4.
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm010037+
CHEMBL413735 219865 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity of human Somatostatin receptor type 4 (hsst4) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 4 (hsst4) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNCCSSCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
CHEMBL219201 216188 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst4Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst4
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccccc2)NC(N)=O)C(=O)N[C@@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm060363v
CHEMBL502511 220934 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CC(=O)N[C@H]1SSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
118718854 122194 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350354 122194 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350907 218305 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)N(C)[C@@H](C(=O)c2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030246p
118719275 122259 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3351044 122259 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL2371070 216787 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N(C)[C@@H](C(=O)c2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030246p
CHEMBL3122124 217882 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysis
ChEMBL None None None CCCC[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2013.12.003
CHEMBL3350883 218285 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]([C@@H](C)c2c[nH]c3ccccc23)NC1=O 10.1021/jm030245x
91936729 174357 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL None None None None 10.1021/jm040794i
CHEMBL430066 174357 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL None None None None 10.1021/jm040794i
42637136 203283 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1074 15 10 13 1.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL563462 203283 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1074 15 10 13 1.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
11828523 201784 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human SSTR4Inhibition of human SSTR4
ChEMBL 669 20 3 9 5.5 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2cnc[nH]2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cccnc1 10.1016/j.bmcl.2010.03.045
CHEMBL54832 201784 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human SSTR4Inhibition of human SSTR4
ChEMBL 669 20 3 9 5.5 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2cnc[nH]2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cccnc1 10.1016/j.bmcl.2010.03.045
11828523 201784 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration required against human Somatostatin receptor type 4Inhibitory concentration required against human Somatostatin receptor type 4
ChEMBL 669 20 3 9 5.5 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2cnc[nH]2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cccnc1 10.1021/jm0205088
CHEMBL54832 201784 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration required against human Somatostatin receptor type 4Inhibitory concentration required against human Somatostatin receptor type 4
ChEMBL 669 20 3 9 5.5 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2cnc[nH]2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cccnc1 10.1021/jm0205088
CHEMBL511086 222371 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(NC(N)=O)cc2)C(N)=O)NC1=O 10.1021/jm701618q
44368398 17038 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1196 16 15 16 -0.2 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1161331 17038 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1196 16 15 16 -0.2 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
25188776 19254 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 551 11 4 4 3.6 NCCCC[C@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1186427 19254 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 551 11 4 4 3.6 NCCCC[C@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL462020 19254 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 551 11 4 4 3.6 NCCCC[C@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
16151826 202635 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1555 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm801314f
CHEMBL558600 202635 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1555 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm801314f
44388121 173501 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1555 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL428295 173501 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1555 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
25189054 19476 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 685 11 4 6 3.0 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCN(S(=O)(=O)c3ccccc3)CC2)C1=O 10.1021/jm801205x
CHEMBL1187568 19476 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 685 11 4 6 3.0 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCN(S(=O)(=O)c3ccccc3)CC2)C1=O 10.1021/jm801205x
CHEMBL509513 19476 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 685 11 4 6 3.0 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCN(S(=O)(=O)c3ccccc3)CC2)C1=O 10.1021/jm801205x
CHEMBL1824058 215821 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2cn(Cc3ccccc3)cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm200307v
56651207 182676 0 None 1 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 655 10 5 9 3.6 NC/C=C/CO[C@@H]1[C@@H](NC(=O)Cc2c[nH]c3ccccc23)COC(=O)c2c(O)cccc2/C=C/COC[C@@H](OCc2ccccc2)[C@H]1O 10.1016/j.ejmech.2018.11.030
CHEMBL4586779 182676 0 None 1 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 655 10 5 9 3.6 NC/C=C/CO[C@@H]1[C@@H](NC(=O)Cc2c[nH]c3ccccc23)COC(=O)c2c(O)cccc2/C=C/COC[C@@H](OCc2ccccc2)[C@H]1O 10.1016/j.ejmech.2018.11.030
CHEMBL525397 222424 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None CC(=O)N[C@H]1CSS[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
44368406 17039 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1022 9 11 12 1.1 C[C@@H]1NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1161332 17039 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1022 9 11 12 1.1 C[C@@H]1NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL262975 217335 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
70689221 84631 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1033 12 13 14 -0.7 C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)N(C)[C@@H](O)NC1=O 10.1021/jm030243c
CHEMBL2093026 84631 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1033 12 13 14 -0.7 C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)N(C)[C@@H](O)NC1=O 10.1021/jm030243c
25187685 19242 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 648 11 4 5 3.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)C2CCN(C(=O)c3ccccc3)CC2)C1=O 10.1021/jm801205x
CHEMBL1186206 19242 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 648 11 4 5 3.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)C2CCN(C(=O)c3ccccc3)CC2)C1=O 10.1021/jm801205x
CHEMBL454202 19242 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 648 11 4 5 3.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)C2CCN(C(=O)c3ccccc3)CC2)C1=O 10.1021/jm801205x
CHEMBL3349507 218191 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL261895 217299 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@H](c1ccc2ccccc2c1)[C@@H]1NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL2372699 217060 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity of human Somatostatin receptor type 4 (hsst4) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 4 (hsst4) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(C(=O)[C@@H](N)Cc2cccc3ccccc23)CCSSCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
44388029 103229 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1659 18 18 20 0.0 CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3I)C(=O)N[C@H]3CCCCCCNC(=O)CC[C@@H](NC(=O)[C@@H](Cc4ccccc4)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC3=O)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049519m
CHEMBL262258 103229 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1659 18 18 20 0.0 CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3I)C(=O)N[C@H]3CCCCCCNC(=O)CC[C@@H](NC(=O)[C@@H](Cc4ccccc4)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC3=O)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049519m
70689723 80743 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1170 16 9 12 4.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL2021559 80743 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1170 16 9 12 4.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL3349664 218227 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC1=O 10.1021/jm970730q
52943613 23742 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 510 11 3 7 3.2 CS[C@@H]1O[C@H](COCc2ccccc2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCN 10.1021/jm1002777
CHEMBL1253788 23742 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 510 11 3 7 3.2 CS[C@@H]1O[C@H](COCc2ccccc2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCN 10.1021/jm1002777
44388124 166149 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1680 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3I)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL410048 166149 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1680 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3I)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
155528330 178119 0 None 1 2 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 513 11 5 7 2.5 Cc1ccc(S[C@H]2O[C@H](CO)[C@@H](O)[C@H](OCCCCN)[C@@H]2NC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.ejmech.2018.11.030
CHEMBL4461404 178119 0 None 1 2 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 513 11 5 7 2.5 Cc1ccc(S[C@H]2O[C@H](CO)[C@@H](O)[C@H](OCCCCN)[C@@H]2NC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.ejmech.2018.11.030
44290734 162614 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity of human Somatostatin receptor type 4 (hsst4) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 4 (hsst4) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL 1123 15 12 11 1.3 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCNC(=O)CCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
CHEMBL406000 162614 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity of human Somatostatin receptor type 4 (hsst4) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 4 (hsst4) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL 1123 15 12 11 1.3 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCNC(=O)CCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
25188780 19203 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 489 10 4 4 2.4 CC(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)NCCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1185941 19203 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 489 10 4 4 2.4 CC(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)NCCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL442605 19203 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 489 10 4 4 2.4 CC(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)NCCc2ccccc2)C1=O 10.1021/jm801205x
25187396 19456 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 475 9 4 4 2.4 CC(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)NCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1187397 19456 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 475 9 4 4 2.4 CC(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)NCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL501699 19456 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 475 9 4 4 2.4 CC(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)NCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL384855 219117 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3I)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(N)=O)CSSC[C@@H](N)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049520l
45273131 201565 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1271 20 11 14 2.8 CN(C(=O)c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(C(N)=O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm801314f
CHEMBL538451 201565 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1271 20 11 14 2.8 CN(C(=O)c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(C(N)=O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm801314f
CHEMBL446077 220722 0 None - 3 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL None None None CNCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm701618q
52947330 23751 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 600 13 4 7 3.6 CS[C@@H]1O[C@H](COCc2ccc(Cl)cc2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCCN=C(N)N 10.1021/jm1002777
CHEMBL1253871 23751 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 600 13 4 7 3.6 CS[C@@H]1O[C@H](COCc2ccc(Cl)cc2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCCN=C(N)N 10.1021/jm1002777
44560873 195926 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL 1809 40 18 25 -1.0 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCOCCOCCOCCNC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL510793 195926 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL 1809 40 18 25 -1.0 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCOCCOCCOCCNC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL2372604 217054 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=5)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=5)
ChEMBL None None None C[C@H](O)[C@@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
CHEMBL2372607 217054 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=5)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=5)
ChEMBL None None None C[C@H](O)[C@@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
16738359 143961 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 641 13 4 4 5.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL374833 143961 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 641 13 4 4 5.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL453938 143961 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 641 13 4 4 5.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm801205x
16738359 143961 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptor
ChEMBL 641 13 4 4 5.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm070246f
CHEMBL374833 143961 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptor
ChEMBL 641 13 4 4 5.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm070246f
CHEMBL453938 143961 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptor
ChEMBL 641 13 4 4 5.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm070246f
155529288 178176 0 None 1 2 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 1072 19 12 13 0.7 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)C(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2018.11.030
CHEMBL4462329 178176 0 None 1 2 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 1072 19 12 13 0.7 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)C(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2018.11.030
16737813 148859 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptor
ChEMBL 418 8 3 3 2.9 NCCCCCN1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
CHEMBL388069 148859 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptor
ChEMBL 418 8 3 3 2.9 NCCCCCN1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
CHEMBL3349669 218232 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL415144 219951 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(N)=O)CSSC[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3I)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049520l
CHEMBL438285 220543 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049519m
90663873 113516 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL 1498 23 21 25 -5.1 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3144283 113516 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL 1498 23 21 25 -5.1 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3144285 113516 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL 1498 23 21 25 -5.1 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
25187398 19220 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 12 4 4 4.0 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1186066 19220 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 12 4 4 4.0 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL448026 19220 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 12 4 4 4.0 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL502777 220936 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL263306 217345 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@H](c1ccc2ccccc2c1)[C@@H]1NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL3350726 218270 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)c(I)c2)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
44368489 17041 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1033 12 13 14 -0.7 C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)N(C)[C@H](O)NC1=O 10.1021/jm030243c
CHEMBL1161334 17041 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1033 12 13 14 -0.7 C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)N(C)[C@H](O)NC1=O 10.1021/jm030243c
CHEMBL524327 222381 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(N)=O)NC1=O 10.1021/jm701618q
44298204 108301 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration required against human Somatostatin receptor type 4Inhibitory concentration required against human Somatostatin receptor type 4
ChEMBL 683 21 3 9 5.5 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)C(OCc2ccccc2)[C@H]1OCCc1cccnc1 10.1021/jm0205088
CHEMBL298149 108301 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration required against human Somatostatin receptor type 4Inhibitory concentration required against human Somatostatin receptor type 4
ChEMBL 683 21 3 9 5.5 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)C(OCc2ccccc2)[C@H]1OCCc1cccnc1 10.1021/jm0205088
CHEMBL505704 220975 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(=O)NO)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
90663874 113517 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL 1660 26 24 30 -7.3 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O[C@@H]4O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]4O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3144286 113517 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL 1660 26 24 30 -7.3 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O[C@@H]4O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]4O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3144291 113517 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL 1660 26 24 30 -7.3 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O[C@@H]4O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]4O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL498985 220868 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
90663867 113512 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL 1322 20 18 20 -3.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)c(I)c2)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O)[C@@H]2O)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm040794i
CHEMBL3144279 113512 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL 1322 20 18 20 -3.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)c(I)c2)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O)[C@@H]2O)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm040794i
CHEMBL412029 219751 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst4Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst4
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC(N)=O)C(=O)N[C@@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm060363v
CHEMBL499760 220880 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL None None None CONC(=O)Nc1ccc(C[C@@H]2NC(=O)[C@H](NC(=O)[C@H](N)Cc3ccc(Cl)cc3)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC2=O)cc1 10.1021/jm701618q
CHEMBL415585 219972 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@H](c1ccc2ccccc2c1)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL3350906 218304 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030246p
CHEMBL415359 219964 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL501282 220915 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL510901 222369 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiography
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701618q
CHEMBL2079559 215974 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2cccc(-c3ccccc3)c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL559150 222523 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm801314f
CHEMBL265836 217445 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049519m
CHEMBL3349678 218240 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
42637069 202288 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1074 15 10 13 1.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL553655 202288 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1074 15 10 13 1.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
44388109 168536 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1653 22 20 21 -0.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCCCC[C@@H](NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@@H]([C@@H](C)O)NC2=O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)O)CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc2ccccc2)C(=O)N3)cc1 10.1021/jm049519m
CHEMBL413924 168536 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1653 22 20 21 -0.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCCCC[C@@H](NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@@H]([C@@H](C)O)NC2=O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)O)CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc2ccccc2)C(=O)N3)cc1 10.1021/jm049519m
2019 10447 0 None -4 10 Human 9.7 pKd = 9.7 Binding
Displacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
44386062 10447 0 None -4 10 Human 9.7 pKd = 9.7 Binding
Displacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
CHEMBL440072 10447 0 None -4 10 Human 9.7 pKd = 9.7 Binding
Displacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
CHEMBL437093 220484 0 None -16 5 Human 6.0 pKd = 6 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N(C)[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm000361p
46865536 18691 0 None -131 7 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 553 6 0 6 5.2 C[C@@H](Cc1ccc2nsnc2c1)CN1C[C@@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)[C@H]2CCCC[C@H]2C1 10.1016/j.bmcl.2010.01.063
CHEMBL1076623 18691 0 None -131 7 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 553 6 0 6 5.2 C[C@@H](Cc1ccc2nsnc2c1)CN1C[C@@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)[C@H]2CCCC[C@H]2C1 10.1016/j.bmcl.2010.01.063
CHEMBL1182658 18691 0 None -131 7 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 553 6 0 6 5.2 C[C@@H](Cc1ccc2nsnc2c1)CN1C[C@@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)[C@H]2CCCC[C@H]2C1 10.1016/j.bmcl.2010.01.063
44565112 19531 0 None -1548 6 Human 5.9 pKd = 5.9 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1187847 19531 0 None -1548 6 Human 5.9 pKd = 5.9 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL523814 19531 0 None -1548 6 Human 5.9 pKd = 5.9 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44565159 201670 0 None -4466 5 Human 5.8 pKd = 5.8 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 497 7 0 7 4.5 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL540705 201670 0 None -4466 5 Human 5.8 pKd = 5.8 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 497 7 0 7 4.5 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
9871544 20988 3 None -30 11 Human 6.8 pKd = 6.8 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)[C@H]3CCCC[C@H]3C2)cn1 10.1016/j.bmcl.2010.01.063
CHEMBL1076624 20988 3 None -30 11 Human 6.8 pKd = 6.8 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)[C@H]3CCCC[C@H]3C2)cn1 10.1016/j.bmcl.2010.01.063
CHEMBL1198948 20988 3 None -30 11 Human 6.8 pKd = 6.8 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)[C@H]3CCCC[C@H]3C2)cn1 10.1016/j.bmcl.2010.01.063
2030 10444 10 None -21379 10 Human 4.8 pKd = 4.8 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
5311377 10444 10 None -21379 10 Human 4.8 pKd = 4.8 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
CHEMBL251541 10444 10 None -21379 10 Human 4.8 pKd = 4.8 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
CHEMBL265636 217437 0 None -12 4 Human 6.7 pKd = 6.7 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccccc2)CSSC[C@@H](C(=O)N(C)[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm000361p
10162564 19312 0 None -4168 8 Human 5.6 pKd = 5.6 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1186652 19312 0 None -4168 8 Human 5.6 pKd = 5.6 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL473763 19312 0 None -4168 8 Human 5.6 pKd = 5.6 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL2370166 216584 0 None -120 5 Human 5.6 pKd = 5.6 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in CHO cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in CHO cells.
ChEMBL None None None C[C@@H](c1ccccc1)N1CC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCNC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C1=O 10.1021/jm970393l
CHEMBL384836 219116 0 None -19 5 Human 6.5 pKd = 6.5 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1C)C(N)=O 10.1021/jm000361p
17955460 183554 0 None -4365 9 Human 5.5 pKd = 5.5 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 491 7 0 4 5.3 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL460542 183554 0 None -4365 9 Human 5.5 pKd = 5.5 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 491 7 0 4 5.3 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL413830 219868 0 None -13 5 Human 6.5 pKd = 6.5 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N(C)[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm000361p
44447073 101325 0 None -9772 10 Human 5.4 pKd = 5.4 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 receptor
ChEMBL 534 2 1 6 3.8 CN1C[C@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL251835 101325 0 None -9772 10 Human 5.4 pKd = 5.4 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 receptor
ChEMBL 534 2 1 6 3.8 CN1C[C@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
46865535 12311 0 None -123 7 Human 6.4 pKd = 6.4 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 550 6 0 5 5.7 Cc1nc2cc(C[C@H](C)CN3C[C@@H](C(=O)N4CCN(c5ccc(F)c(F)c5)CC4)[C@H]4CCCC[C@H]4C3)ccc2o1 10.1016/j.bmcl.2010.01.063
CHEMBL1076622 12311 0 None -123 7 Human 6.4 pKd = 6.4 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 550 6 0 5 5.7 Cc1nc2cc(C[C@H](C)CN3C[C@@H](C(=O)N4CCN(c5ccc(F)c(F)c5)CC4)[C@H]4CCCC[C@H]4C3)ccc2o1 10.1016/j.bmcl.2010.01.063
CHEMBL2370167 216585 0 None -1905 5 Human 5.4 pKd = 5.4 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in CHO cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in CHO cells.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCNC(=O)[C@@H](N)Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN([C@H](C)c2ccccc2)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm970393l
CHEMBL2370168 216586 0 None -1023 5 Human 5.3 pKd = 5.3 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in CHO cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in CHO cells.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCNC(=O)[C@@H](N)Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm970393l
9849682 101727 0 None -23988 10 Human 5.3 pKd = 5.3 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 receptor
ChEMBL 523 2 1 5 2.9 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL254500 101727 0 None -23988 10 Human 5.3 pKd = 5.3 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 receptor
ChEMBL 523 2 1 5 2.9 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
155544425 180161 0 None -251188 5 Human 5.3 pKd = 5.3 Binding
Displacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL 1785 27 15 26 3.3 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSC[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc3ccccc3)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O)[C@@]1(C)O[C@H]1[C@H](C)[C@@H]1C[C@@](O)(NC(=O)O1)[C@H](OC)/C=C/C=C(\C)C2 10.1021/acs.jmedchem.8b02036
CHEMBL4527856 180161 0 None -251188 5 Human 5.3 pKd = 5.3 Binding
Displacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL 1785 27 15 26 3.3 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSC[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc3ccccc3)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O)[C@@]1(C)O[C@H]1[C@H](C)[C@@H]1C[C@@](O)(NC(=O)O1)[C@H](OC)/C=C/C=C(\C)C2 10.1021/acs.jmedchem.8b02036
44447078 101392 0 None -30 7 Human 5.3 pKd = 5.3 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 receptor
ChEMBL 534 2 1 6 3.8 CN1C[C@@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@H]2c3cccc4[nH]c(Br)c(c34)C[C@@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252232 101392 0 None -30 7 Human 5.3 pKd = 5.3 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 receptor
ChEMBL 534 2 1 6 3.8 CN1C[C@@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@H]2c3cccc4[nH]c(Br)c(c34)C[C@@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL409019 219521 0 None -20 5 Human 6.2 pKd = 6.2 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1C)C(N)=O 10.1021/jm000361p
46880588 20989 0 None -8 7 Human 5.2 pKd = 5.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@@H](C)CN2C[C@H]3CCCC[C@H]3[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)C2)cn1 10.1016/j.bmcl.2010.01.063
CHEMBL1076625 20989 0 None -8 7 Human 5.2 pKd = 5.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@@H](C)CN2C[C@H]3CCCC[C@H]3[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)C2)cn1 10.1016/j.bmcl.2010.01.063
CHEMBL1198974 20989 0 None -8 7 Human 5.2 pKd = 5.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@@H](C)CN2C[C@H]3CCCC[C@H]3[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)C2)cn1 10.1016/j.bmcl.2010.01.063
44447077 101391 0 None -19 7 Human 5.1 pKd = 5.1 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 receptor
ChEMBL 523 2 1 5 2.9 CN1C[C@@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@H]2c3cccc4[nH]c(Br)c(c34)C[C@@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252231 101391 0 None -19 7 Human 5.1 pKd = 5.1 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 receptor
ChEMBL 523 2 1 5 2.9 CN1C[C@@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@H]2c3cccc4[nH]c(Br)c(c34)C[C@@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL421362 220053 0 None -6606 5 Human 5.1 pKd = 5.1 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in CHO cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in CHO cells.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm970393l
168272497 197012 0 None 3467 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 448 8 2 4 5.1 Fc1ccc2c(Cc3nnc(Cc4cccc(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5174969 197012 0 None 3467 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 448 8 2 4 5.1 Fc1ccc2c(Cc3nnc(Cc4cccc(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
168280914 197581 0 None 18197 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5183772 197581 0 None 18197 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
168288485 198510 0 None 2454 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 430 8 2 4 5.0 Clc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5197201 198510 0 None 2454 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 430 8 2 4 5.0 Clc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
16129706 215810 40 None -13 5 Human 9.2 pKi = 9.2 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 receptor expressed in CHO cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/s0960-894x(01)00107-x
CHEMBL1823872 215810 40 None -13 5 Human 9.2 pKi = 9.2 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 receptor expressed in CHO cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/s0960-894x(01)00107-x
168279197 197711 0 None 1621 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5185547 197711 0 None 1621 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
16129706 215810 40 None -13 5 Human 9.2 pKi = 9.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0108449
CHEMBL1823872 215810 40 None -13 5 Human 9.2 pKi = 9.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0108449
2082 9039 14 None 7079 2 Human 9.2 pKi = 9.2 Binding
Displacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting methodDisplacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting method
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1039/C8MD00388B
5311374 9039 14 None 7079 2 Human 9.2 pKi = 9.2 Binding
Displacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting methodDisplacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting method
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1039/C8MD00388B
CHEMBL1450103 9039 14 None 7079 2 Human 9.2 pKi = 9.2 Binding
Displacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting methodDisplacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting method
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1039/C8MD00388B
168274800 196871 0 None 630 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 2 6 3.8 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5172814 196871 0 None 630 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 2 6 3.8 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471832 197054 0 None 138 5 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 471 8 3 4 5.1 Fc1ccc2c(Cc3nnc(Cc4c[nH]c5cc(F)ccc45)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5175637 197054 0 None 138 5 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 471 8 3 4 5.1 Fc1ccc2c(Cc3nnc(Cc4c[nH]c5cc(F)ccc45)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
168271257 197293 0 None 8912 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1ccccc1Cc1nnc(Cc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5179456 197293 0 None 8912 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1ccccc1Cc1nnc(Cc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
142471936 198274 0 None 776 5 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 482 8 2 4 5.5 Fc1ccc2c(Cc3nnc(Cc4cccc(C(F)(F)F)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5193727 198274 0 None 776 5 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 482 8 2 4 5.5 Fc1ccc2c(Cc3nnc(Cc4cccc(C(F)(F)F)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
16129706 215810 40 None -13 5 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-somatostatin from human SSTR4 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR4 expressed in CHO-K1 cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2013.11.065
CHEMBL1823872 215810 40 None -13 5 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-somatostatin from human SSTR4 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR4 expressed in CHO-K1 cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2013.11.065
142471730 197164 0 None 741 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 464 8 2 4 5.3 FC(F)(F)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5177487 197164 0 None 741 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 464 8 2 4 5.3 FC(F)(F)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
168272821 197373 0 None 4677 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 464 8 2 4 5.6 Clc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl 10.1039/D1MD00044F
CHEMBL5180543 197373 0 None 4677 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 464 8 2 4 5.6 Clc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl 10.1039/D1MD00044F
142471924 197173 0 None 524 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 432 8 2 4 4.6 Fc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5177573 197173 0 None 524 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 432 8 2 4 4.6 Fc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
168296886 199286 0 None 5754 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1ccccc1Cc1nnc(Cc2c[nH]c3cc(F)ccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5209180 199286 0 None 5754 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1ccccc1Cc1nnc(Cc2c[nH]c3cc(F)ccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
142471678 196821 0 None 660 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 474 9 2 6 3.7 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5171935 196821 0 None 660 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 474 9 2 6 3.7 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471848 198046 0 None 263 4 Human 9.0 pKi = 9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 8 2 4 5.2 Fc1ccc2c(Cc3nnc(Cc4cccc(Br)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5190457 198046 0 None 263 4 Human 9.0 pKi = 9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 8 2 4 5.2 Fc1ccc2c(Cc3nnc(Cc4cccc(Br)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
168275406 197086 0 None 794 4 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 482 8 2 4 5.7 Fc1ccc2c(Cc3nnc(Cc4ccc(Cl)c(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5176083 197086 0 None 794 4 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 482 8 2 4 5.7 Fc1ccc2c(Cc3nnc(Cc4ccc(Cl)c(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
10115 8891 14 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-LTT-SRIF-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 60 mins by scintillation counting methodDisplacement of [125I]-LTT-SRIF-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 60 mins by scintillation counting method
ChEMBL 468 10 4 5 1.4 NCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NS(=O)(=O)c1ccc(c2c1cccc2)C 10.1039/C8MD00388B
11442741 8891 14 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-LTT-SRIF-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 60 mins by scintillation counting methodDisplacement of [125I]-LTT-SRIF-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 60 mins by scintillation counting method
ChEMBL 468 10 4 5 1.4 NCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NS(=O)(=O)c1ccc(c2c1cccc2)C 10.1039/C8MD00388B
CHEMBL4451852 8891 14 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-LTT-SRIF-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 60 mins by scintillation counting methodDisplacement of [125I]-LTT-SRIF-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 60 mins by scintillation counting method
ChEMBL 468 10 4 5 1.4 NCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NS(=O)(=O)c1ccc(c2c1cccc2)C 10.1039/C8MD00388B
168279055 198019 0 None 4265 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 464 8 2 4 5.6 Clc1cc(Cl)cc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5190056 198019 0 None 4265 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 464 8 2 4 5.6 Clc1cc(Cl)cc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
16129706 215810 40 None -13 5 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm021093t
CHEMBL1823872 215810 40 None -13 5 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm021093t
CHEMBL4299281 220337 0 None -44 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting methodDisplacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting method
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](C)NC(=O)[C@H]1CCCN1C(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.ejmech.2016.02.046
142471891 197374 0 None 436 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 430 8 2 4 5.0 Clc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5180551 197374 0 None 436 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 430 8 2 4 5.0 Clc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
16129706 215810 40 None -13 5 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm980118e
CHEMBL1823872 215810 40 None -13 5 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm980118e
16129706 215810 40 None -13 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards somatostatin receptor type 4Binding affinity towards somatostatin receptor type 4
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm050376t
CHEMBL1823872 215810 40 None -13 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards somatostatin receptor type 4Binding affinity towards somatostatin receptor type 4
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm050376t
168275268 196937 0 None 2884 2 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 482 8 2 4 5.7 Fc1ccc2c(Cc3nnc(Cc4cc(Cl)cc(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5173784 196937 0 None 2884 2 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 482 8 2 4 5.7 Fc1ccc2c(Cc3nnc(Cc4cc(Cl)cc(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
142471929 197946 0 None 676 2 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 414 8 2 4 4.4 Fc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5188841 197946 0 None 676 2 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 414 8 2 4 4.4 Fc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471978 199222 0 None 891 2 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 396 8 2 4 4.3 c1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5208396 199222 0 None 891 2 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 396 8 2 4 4.3 c1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
16129706 215810 40 None -13 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards Somatostatin receptor type 4 (hsst4)Binding affinity towards Somatostatin receptor type 4 (hsst4)
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm020424z
CHEMBL1823872 215810 40 None -13 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards Somatostatin receptor type 4 (hsst4)Binding affinity towards Somatostatin receptor type 4 (hsst4)
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm020424z
CHEMBL408362 219489 0 None -44 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human sst4 receptor expressed in CHO-K1 cellsBinding affinity towards human sst4 receptor expressed in CHO-K1 cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm980194h
CHEMBL3098601 217797 0 None -8 5 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-somatostatin from human SSTR4 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR4 expressed in CHO-K1 cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1C/C=C\C[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2013.11.065
142471801 199078 0 None 199 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 494 9 2 5 5.3 COc1ccc2[nH]cc(Cc3nnc(Cc4cccc(C(F)(F)F)c4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
CHEMBL5206148 199078 0 None 199 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 494 9 2 5 5.3 COc1ccc2[nH]cc(Cc3nnc(Cc4cccc(C(F)(F)F)c4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
91809283 132538 0 None -134 6 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1456 23 17 16 2.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3647684 132538 0 None -134 6 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1456 23 17 16 2.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
10009650 106571 0 None 3 4 Human 7.0 pKi = 7 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
ChEMBL 668 20 3 8 6.1 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL285333 106571 0 None 3 4 Human 7.0 pKi = 7 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
ChEMBL 668 20 3 8 6.1 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
44298251 201450 0 None - 1 Human 7.0 pKi = 7 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 668 20 3 8 6.1 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)C(OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm0205088
CHEMBL53204 201450 0 None - 1 Human 7.0 pKi = 7 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 668 20 3 8 6.1 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)C(OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm0205088
CHEMBL2311098 216284 0 None -83 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369733 216440 0 None -5 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N(C)[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369735 216442 0 None -181 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369749 216446 0 None -83 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369750 216447 0 None -27 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None CN[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC1=O 10.1021/jm0005048
CHEMBL2369751 216448 0 None -11 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H]1CSSC[C@H](N(C)C(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2cccnc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]([C@H](C)O)C(=O)N1 10.1021/jm0005048
CHEMBL2369752 216449 0 None -19 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369753 216450 0 None -11 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@@H]1C(=O)N[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccnc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N1C 10.1021/jm0005048
CHEMBL2369754 216451 0 None -107 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369755 216452 0 None -165 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369756 216453 0 None -5 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)N(C)C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369757 216454 0 None -40 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2cccnc2)CSSC[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369758 216455 0 None -36 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369759 216456 0 None -1 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)C(N)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369760 216457 0 None -42 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@@H](N)CCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369761 216458 0 None -8 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None CNC(=O)[C@@H](NC(=O)[C@@H]1CSSC[C@@H](N(C)C(=O)C(N)Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccnc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]([C@H](C)O)C(=O)N1)C(c1ccccc1)c1ccccc1 10.1021/jm0005048
10625762 44158 0 None -1 2 Human 6.0 pKi = 6 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 517 11 3 4 5.2 NCCCC/N=C(\S)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL145472 44158 0 None -1 2 Human 6.0 pKi = 6 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 517 11 3 4 5.2 NCCCC/N=C(\S)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
10554709 126092 0 None 3 2 Human 6.0 pKi = 6 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 549 7 3 5 5.4 S=C(NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)Nc1ccc2[nH]nnc2c1 10.1021/jm980118e
CHEMBL344074 126092 0 None 3 2 Human 6.0 pKi = 6 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 549 7 3 5 5.4 S=C(NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)Nc1ccc2[nH]nnc2c1 10.1021/jm980118e
90665461 116038 0 None -5 5 Human 5.0 pKi = 5 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 807 13 3 7 4.3 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CCC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
CHEMBL3218123 116038 0 None -5 5 Human 5.0 pKi = 5 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 807 13 3 7 4.3 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CCC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
10876118 203032 0 None - 1 Human 6.0 pKi = 6.0 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 668 20 3 8 6.1 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1c[nH]cn1 10.1021/jm0205088
CHEMBL56181 203032 0 None - 1 Human 6.0 pKi = 6.0 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 668 20 3 8 6.1 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1c[nH]cn1 10.1021/jm0205088
CHEMBL275806 217602 0 None -6 4 Human 6.0 pKi = 6.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)O)NC1=O 10.1021/jm9806289
90644981 118590 0 None -660 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]SS28 from human SST5 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS28 from human SST5 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 365 5 3 2 4.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287613 118590 0 None -660 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]SS28 from human SST5 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS28 from human SST5 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 365 5 3 2 4.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
142471719 197281 0 None 204 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 1 5 5.5 Cn1cc(CCc2nnc(Cc3cccc(C(F)(F)F)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
CHEMBL5179321 197281 0 None 204 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 1 5 5.5 Cn1cc(CCc2nnc(Cc3cccc(C(F)(F)F)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
9852911 106159 0 None -8 6 Human 6.0 pKi = 6.0 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL282618 106159 0 None -8 6 Human 6.0 pKi = 6.0 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccc1 10.1021/jm9800346
9852911 106159 0 None -8 6 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccc1 10.1016/j.ejmech.2018.11.030
CHEMBL282618 106159 0 None -8 6 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccc1 10.1016/j.ejmech.2018.11.030
10815650 171711 0 None - 1 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 512 12 3 5 4.6 S=C(NCCCNc1ccccn1)NCCCN(Cc1ccc(Br)cc1)c1ccccn1 10.1021/jm980118e
CHEMBL422475 171711 0 None - 1 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 512 12 3 5 4.6 S=C(NCCCNc1ccccn1)NCCCN(Cc1ccc(Br)cc1)c1ccccn1 10.1021/jm980118e
127029955 145664 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting methodDisplacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting method
ChEMBL 391 6 1 3 5.3 NCCCc1cc(Cl)cc2c(=O)cc(CCc3cccc4ccccc34)oc12 10.1016/j.ejmech.2016.02.046
CHEMBL3780791 145664 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting methodDisplacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting method
ChEMBL 391 6 1 3 5.3 NCCCc1cc(Cl)cc2c(=O)cc(CCc3cccc4ccccc34)oc12 10.1016/j.ejmech.2016.02.046
CHEMBL3782073 145664 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting methodDisplacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting method
ChEMBL 391 6 1 3 5.3 NCCCc1cc(Cl)cc2c(=O)cc(CCc3cccc4ccccc34)oc12 10.1016/j.ejmech.2016.02.046
9872511 128797 0 None 21 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 486 11 3 4 4.1 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Br)cc1)c1ccccn1 10.1021/jm980118e
CHEMBL359453 128797 0 None 21 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 486 11 3 4 4.1 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Br)cc1)c1ccccn1 10.1021/jm980118e
142471938 198787 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 410 9 2 4 4.5 c1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5201594 198787 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 410 9 2 4 4.5 c1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471860 199284 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 428 9 2 4 4.6 Fc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5209165 199284 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 428 9 2 4 4.6 Fc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
10603005 125916 0 None - 1 Human 5.9 pKi = 5.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 562 8 3 4 5.7 S=C(NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCc1nc2ccccc2[nH]1 10.1021/jm980118e
CHEMBL342781 125916 0 None - 1 Human 5.9 pKi = 5.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 562 8 3 4 5.7 S=C(NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCc1nc2ccccc2[nH]1 10.1021/jm980118e
10974575 107571 0 None - 1 Human 5.9 pKi = 5.9 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 713 20 2 8 7.4 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccc(Cl)nc1 10.1021/jm0205088
CHEMBL293114 107571 0 None - 1 Human 5.9 pKi = 5.9 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 713 20 2 8 7.4 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccc(Cl)nc1 10.1021/jm0205088
90665463 116039 0 None -4 5 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 882 28 3 9 4.5 COC(=O)CCN(Cc1ccccc1)C(=O)CCN(C[C@@H](C)O)C(=O)CCN(CCCCN)C(=O)CCN(CCc1c[nH]c2ccccc12)C(=O)CCN(Cc1ccccc1)C(C)=O 10.1039/C2MD20265D
CHEMBL3218124 116039 0 None -4 5 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 882 28 3 9 4.5 COC(=O)CCN(Cc1ccccc1)C(=O)CCN(C[C@@H](C)O)C(=O)CCN(CCCCN)C(=O)CCN(CCc1c[nH]c2ccccc12)C(=O)CCN(Cc1ccccc1)C(C)=O 10.1039/C2MD20265D
CHEMBL1791312 215704 0 None -123 2 Human 6.9 pKi = 6.9 Binding
Inhibition of human somatostatin receptor type 4Inhibition of human somatostatin receptor type 4
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@H](Cc2cnccn2)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm058184l
CHEMBL2371893 216926 0 None -112 5 Human 5.9 pKi = 5.9 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(C(F)(F)F)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
10865371 107851 0 None - 1 Human 5.9 pKi = 5.9 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 693 20 2 8 7.1 Cc1ccc(CO[C@H]2[C@H](OCc3ccccc3)[C@@H](OCc3ccccc3)[C@H](OCCc3c[nH]c4ccccc34)O[C@@H]2COCCCCCN)cn1 10.1021/jm0205088
CHEMBL294830 107851 0 None - 1 Human 5.9 pKi = 5.9 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 693 20 2 8 7.1 Cc1ccc(CO[C@H]2[C@H](OCc3ccccc3)[C@@H](OCc3ccccc3)[C@H](OCCc3c[nH]c4ccccc34)O[C@@H]2COCCCCCN)cn1 10.1021/jm0205088
44397648 73538 0 None -32 5 Human 6.9 pKi = 6.9 Binding
Binding affinity against human sst4 receptor at a dose of 10 uMBinding affinity against human sst4 receptor at a dose of 10 uM
ChEMBL 476 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3c(Cl)cccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL185861 73538 0 None -32 5 Human 6.9 pKi = 6.9 Binding
Binding affinity against human sst4 receptor at a dose of 10 uMBinding affinity against human sst4 receptor at a dose of 10 uM
ChEMBL 476 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3c(Cl)cccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
10650940 128762 0 None 5 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 582 13 3 4 6.1 S=C(NCCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCCc1c[nH]cn1 10.1021/jm980118e
CHEMBL359215 128762 0 None 5 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 582 13 3 4 6.1 S=C(NCCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCCc1c[nH]cn1 10.1021/jm980118e
10436888 126089 0 None 295 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 524 10 3 4 4.8 O=C(NCCCc1c[nH]cn1)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL344059 126089 0 None 295 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 524 10 3 4 4.8 O=C(NCCCc1c[nH]cn1)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
142471961 198200 0 None 275 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 494 10 2 5 5.4 FC(F)(F)Oc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5192791 198200 0 None 275 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 494 10 2 5 5.4 FC(F)(F)Oc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
44397706 73965 0 None -77 5 Human 6.9 pKi = 6.9 Binding
Binding affinity against human sst4 receptor at a dose of 10 uMBinding affinity against human sst4 receptor at a dose of 10 uM
ChEMBL 456 9 2 6 5.4 Cc1cccc2c(CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
CHEMBL187768 73965 0 None -77 5 Human 6.9 pKi = 6.9 Binding
Binding affinity against human sst4 receptor at a dose of 10 uMBinding affinity against human sst4 receptor at a dose of 10 uM
ChEMBL 456 9 2 6 5.4 Cc1cccc2c(CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
10745635 126125 0 None 1 2 Human 5.9 pKi = 5.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 568 12 2 5 5.7 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCCn1ccnc1 10.1021/jm980118e
CHEMBL344285 126125 0 None 1 2 Human 5.9 pKi = 5.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 568 12 2 5 5.7 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCCn1ccnc1 10.1021/jm980118e
10053855 175333 0 None -263 2 Human 5.9 pKi = 5.9 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 5 (hSSTR-5)In vitro binding affinity was evaluated against human Somatostatin receptor type 5 (hSSTR-5)
ChEMBL 574 8 2 6 3.2 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N(C)C[C@H]1OC[C@H](N)CO1)N1CCN(C2CCCN(c3ccccc3)C2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL435631 175333 0 None -263 2 Human 5.9 pKi = 5.9 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 5 (hSSTR-5)In vitro binding affinity was evaluated against human Somatostatin receptor type 5 (hSSTR-5)
ChEMBL 574 8 2 6 3.2 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N(C)C[C@H]1OC[C@H](N)CO1)N1CCN(C2CCCN(c3ccccc3)C2)C1=O 10.1016/s0960-894x(99)00016-5
155519582 177165 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 464 8 2 4 5.4 Clc1ccc(Cn2c(CCc3c[nH]cn3)nnc2CCc2c[nH]c3ccccc23)cc1Cl 10.1039/C8MD00388B
CHEMBL4447896 177165 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 464 8 2 4 5.4 Clc1ccc(Cn2c(CCc3c[nH]cn3)nnc2CCc2c[nH]c3ccccc23)cc1Cl 10.1039/C8MD00388B
CHEMBL2372960 217105 0 None -4 4 Human 6.8 pKi = 6.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
ChEMBL None None None CC(C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O)C1CCCS1 10.1021/jm9806289
9893924 11520 34 None 52 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1039/C8MD00388B
CHEMBL103769 11520 34 None 52 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1039/C8MD00388B
10698706 40582 0 None - 1 Human 4.8 pKi = 4.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 591 8 2 4 7.1 S=C(NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)Nc1ccc(N2CCCCC2)cc1 10.1021/jm980118e
CHEMBL142293 40582 0 None - 1 Human 4.8 pKi = 4.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 591 8 2 4 7.1 S=C(NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)Nc1ccc(N2CCCCC2)cc1 10.1021/jm980118e
CHEMBL408987 219519 0 None -9 5 Human 5.8 pKi = 5.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)CNC1=O 10.1021/jm9806289
2054 10746 15 None -446 11 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
71306 10746 15 None -446 11 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL264186 10746 15 None -446 11 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL3349523 10746 15 None -446 11 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
DB04894 10746 15 None -446 11 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL437220 220490 0 None -63 4 Human 5.8 pKi = 5.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
10369961 41413 0 None 48 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 536 11 3 4 5.2 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1cccc2ccccc12)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL142986 41413 0 None 48 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 536 11 3 4 5.2 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1cccc2ccccc12)c1ccc(Br)cn1 10.1021/jm980118e
142471896 197922 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 446 9 2 4 4.8 Fc1cc(F)cc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5188361 197922 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 446 9 2 4 4.8 Fc1cc(F)cc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
44820545 59268 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 519 11 3 3 5.3 S=C(NCCCc1cnc[nH]1)NCCCN(Cc1ccc(Cl)cc1)c1ccc(Br)cc1 10.1039/c1md00200g
CHEMBL1591395 59268 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 519 11 3 3 5.3 S=C(NCCCc1cnc[nH]1)NCCCN(Cc1ccc(Cl)cc1)c1ccc(Br)cc1 10.1039/c1md00200g
CHEMBL2372957 217102 0 None -85 4 Human 5.8 pKi = 5.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
ChEMBL None None None C[C@@H](C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(N)=O)NC1=O)C1CCCS1 10.1021/jm9806289
9852911 106159 0 None -8 6 Human 5.8 pKi = 5.8 Binding
Binding affinity to sst4 receptor (unknown origin)Binding affinity to sst4 receptor (unknown origin)
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccc1 10.1016/j.ejmech.2016.02.046
CHEMBL282618 106159 0 None -8 6 Human 5.8 pKi = 5.8 Binding
Binding affinity to sst4 receptor (unknown origin)Binding affinity to sst4 receptor (unknown origin)
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccc1 10.1016/j.ejmech.2016.02.046
9852911 106159 0 None -8 6 Human 5.8 pKi = 5.8 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccc1 10.1021/jm0205088
CHEMBL282618 106159 0 None -8 6 Human 5.8 pKi = 5.8 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccc1 10.1021/jm0205088
9893924 11520 34 None 52 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1039/c1md00200g
CHEMBL103769 11520 34 None 52 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1039/c1md00200g
9985523 105937 0 None 1 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
ChEMBL 572 17 2 6 6.2 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)C[C@@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL281200 105937 0 None 1 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
ChEMBL 572 17 2 6 6.2 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)C[C@@H]1OCc1ccccc1 10.1021/jm9800346
10816544 40584 0 None 43 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 551 10 2 4 5.6 S=C(NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCc1ccccn1 10.1021/jm980118e
CHEMBL142295 40584 0 None 43 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 551 10 2 4 5.6 S=C(NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCc1ccccn1 10.1021/jm980118e
10650427 41209 0 None 1 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 554 11 2 5 5.3 S=C(NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCCn1ccnc1 10.1021/jm980118e
CHEMBL142823 41209 0 None 1 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 554 11 2 5 5.3 S=C(NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCCn1ccnc1 10.1021/jm980118e
10625454 126142 0 None 2 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 507 11 3 6 4.5 O=[N+]([O-])c1ccc(N(CC/N=C(\S)NCCCc2c[nH]cn2)Cc2ccc(Cl)c(Cl)c2)nc1 10.1021/jm980118e
CHEMBL344404 126142 0 None 2 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 507 11 3 6 4.5 O=[N+]([O-])c1ccc(N(CC/N=C(\S)NCCCc2c[nH]cn2)Cc2ccc(Cl)c(Cl)c2)nc1 10.1021/jm980118e
CHEMBL413171 219830 0 None -1 5 Human 6.8 pKi = 6.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2c(F)c(F)c(F)c(F)c2F)CSSC[C@H](C(=O)N[C@@H](Cc2c(F)c(F)c(F)c(F)c2F)C(N)=O)NC1=O 10.1021/jm9806289
10698494 41719 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 580 12 3 5 5.9 S=C(NCCCNc1ccccn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL143245 41719 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 580 12 3 5 5.9 S=C(NCCCNc1ccccn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
44820569 59252 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 534 11 2 4 5.1 CN(CCCN(Cc1ccc(Cl)cc1)c1ccc(Br)cn1)C(=S)NCCCc1cnc[nH]1 10.1039/c1md00200g
CHEMBL1591268 59252 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 534 11 2 4 5.1 CN(CCCN(Cc1ccc(Cl)cc1)c1ccc(Br)cn1)C(=S)NCCCc1cnc[nH]1 10.1039/c1md00200g
56945132 178199 0 None 251 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 478 9 2 4 5.8 Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl 10.1039/C8MD00388B
CHEMBL4462793 178199 0 None 251 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 478 9 2 4 5.8 Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl 10.1039/C8MD00388B
10770814 107569 0 None 1 5 Human 5.7 pKi = 5.7 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL29311 107569 0 None 1 5 Human 5.7 pKi = 5.7 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
155546680 180344 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 628 16 1 5 8.3 NCCCCC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1Cc1cccc2ccccc12 10.1016/j.ejmech.2018.11.030
CHEMBL4532486 180344 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 628 16 1 5 8.3 NCCCCC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1Cc1cccc2ccccc12 10.1016/j.ejmech.2018.11.030
56651206 181410 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 659 11 5 9 3.8 NCCCCO[C@@H]1[C@@H](NC(=O)Cc2c[nH]c3ccccc23)COC(=O)c2c(O)cccc2CCCOC[C@@H](OCc2ccccc2)[C@H]1O 10.1016/j.ejmech.2018.11.030
CHEMBL4557933 181410 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 659 11 5 9 3.8 NCCCCO[C@@H]1[C@@H](NC(=O)Cc2c[nH]c3ccccc23)COC(=O)c2c(O)cccc2CCCOC[C@@H](OCc2ccccc2)[C@H]1O 10.1016/j.ejmech.2018.11.030
122181227 128624 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4
ChEMBL 628 16 1 5 8.3 NCCCCC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1Cc1ccc2ccccc2c1 10.1039/C4MD00074A
CHEMBL3589942 128624 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4
ChEMBL 628 16 1 5 8.3 NCCCCC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1Cc1ccc2ccccc2c1 10.1039/C4MD00074A
13690207 122160 0 None -2041 5 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm980118e
CHEMBL3350037 122160 0 None -2041 5 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm980118e
CHEMBL1794035 215716 0 None -7 5 Human 8.7 pKi = 8.7 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm0005048
91809287 167037 0 None -41 6 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1472 23 17 16 1.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCC[S@+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL4110066 167037 0 None -41 6 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1472 23 17 16 1.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCC[S@+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
142471684 198231 0 None 1174 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5193172 198231 0 None 1174 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
155541853 179822 0 None -3 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 1636 26 21 23 -3.8 CC(=O)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1039/C8MD00388B
CHEMBL4519096 179822 0 None -3 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 1636 26 21 23 -3.8 CC(=O)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1039/C8MD00388B
168296234 199067 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 430 8 2 4 5.0 Clc1ccccc1Cc1nnc(Cc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5205998 199067 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 430 8 2 4 5.0 Clc1ccccc1Cc1nnc(Cc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
142471841 198364 0 None 363 3 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1ccc2[nH]cc(Cc3nnc(Cc4ccc(F)cc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
CHEMBL5195145 198364 0 None 363 3 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1ccc2[nH]cc(Cc3nnc(Cc4ccc(F)cc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
91809286 132541 0 None -128 6 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1489 23 16 15 2.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCS(=O)(=O)C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL3647687 132541 0 None -128 6 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1489 23 16 15 2.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCS(=O)(=O)C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
10699714 106193 0 None 1 5 Human 5.7 pKi = 5.7 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL282803 106193 0 None 1 5 Human 5.7 pKi = 5.7 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
10325243 107271 0 None 1 5 Human 5.7 pKi = 5.7 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
ChEMBL 549 17 1 7 5.3 CO[C@@H]1O[C@H](COCCCCCN)[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL29102 107271 0 None 1 5 Human 5.7 pKi = 5.7 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
ChEMBL 549 17 1 7 5.3 CO[C@@H]1O[C@H](COCCCCCN)[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
44308969 211143 0 None -1258 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human sst4 receptor expressed in CHO-K1 cellsBinding affinity towards human sst4 receptor expressed in CHO-K1 cells
ChEMBL 539 7 4 3 4.7 NC[C@@H]1CCC[C@H](CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm980194h
CHEMBL71723 211143 0 None -1258 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human sst4 receptor expressed in CHO-K1 cellsBinding affinity towards human sst4 receptor expressed in CHO-K1 cells
ChEMBL 539 7 4 3 4.7 NC[C@@H]1CCC[C@H](CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm980194h
10601454 42083 0 None -1 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 499 11 3 4 5.0 NCCCC/N=C(\S)NCCCN(Cc1cccc2ccccc12)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL143668 42083 0 None -1 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 499 11 3 4 5.0 NCCCC/N=C(\S)NCCCN(Cc1cccc2ccccc12)c1ccc(Br)cn1 10.1021/jm980118e
90665458 116035 0 None -2 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 632 11 3 6 2.5 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
CHEMBL3218120 116035 0 None -2 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 632 11 3 6 2.5 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
155550820 181068 0 None -5 2 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 1275 22 16 18 -2.3 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)C(C)C)NC(=O)[C@H](CC(=O)N[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2NC(C)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2018.11.030
CHEMBL4549840 181068 0 None -5 2 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 1275 22 16 18 -2.3 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)C(C)C)NC(=O)[C@H](CC(=O)N[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2NC(C)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2018.11.030
127032867 145648 0 None 2 2 Human 5.7 pKi = 5.7 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 338 10 2 3 4.3 NCCCCCOc1ccccc1OCCc1c[nH]c2ccccc12 10.1016/j.ejmech.2016.02.046
CHEMBL3781875 145648 0 None 2 2 Human 5.7 pKi = 5.7 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 338 10 2 3 4.3 NCCCCCOc1ccccc1OCCc1c[nH]c2ccccc12 10.1016/j.ejmech.2016.02.046
155558366 181517 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 410 9 2 4 4.3 c1ccc(CCn2c(CCc3c[nH]cn3)nnc2CCc2c[nH]c3ccccc23)cc1 10.1039/C8MD00388B
CHEMBL4560435 181517 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 410 9 2 4 4.3 c1ccc(CCn2c(CCc3c[nH]cn3)nnc2CCc2c[nH]c3ccccc23)cc1 10.1039/C8MD00388B
127033186 145656 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-SRIF14 from human sst4 receptorDisplacement of [125I]-SRIF14 from human sst4 receptor
ChEMBL 779 17 5 9 6.1 CC(C)CC[C@]1(Cc2ccccc2)NC=C([C@@]2(Cc3ccccc3)NC=C([C@]3(CCCN)NC=C([C@@]4(CC(C)C)NC=C(Cc5ccccc5)C4=O)C3=O)C2=O)C1=O 10.1016/j.ejmech.2016.02.046
CHEMBL3782021 145656 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-SRIF14 from human sst4 receptorDisplacement of [125I]-SRIF14 from human sst4 receptor
ChEMBL 779 17 5 9 6.1 CC(C)CC[C@]1(Cc2ccccc2)NC=C([C@@]2(Cc3ccccc3)NC=C([C@]3(CCCN)NC=C([C@@]4(CC(C)C)NC=C(Cc5ccccc5)C4=O)C3=O)C2=O)C1=O 10.1016/j.ejmech.2016.02.046
142471846 198108 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 4 5.1 Clc1ccccc1Cc1nnc(CCc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5191532 198108 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 4 5.1 Clc1ccccc1Cc1nnc(CCc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
155553012 180865 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 511 10 5 7 2.3 Cc1ccc(S[C@H]2O[C@H](CO)[C@@H](O)[C@H](OC/C=C/CN)[C@@H]2NC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.ejmech.2018.11.030
CHEMBL4544582 180865 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 511 10 5 7 2.3 Cc1ccc(S[C@H]2O[C@H](CO)[C@@H](O)[C@H](OC/C=C/CN)[C@@H]2NC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.ejmech.2018.11.030
90665462 116007 0 None -6 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 867 27 3 9 4.1 COC(=O)CCN(Cc1ccccc1)C(=O)CCN(C[C@@H](C)O)C(=O)CCN(CCCCN)C(=O)CN(CCc1c[nH]c2ccccc12)C(=O)CCN(Cc1ccccc1)C(C)=O 10.1039/C2MD20265D
CHEMBL3217760 116007 0 None -6 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 867 27 3 9 4.1 COC(=O)CCN(Cc1ccccc1)C(=O)CCN(C[C@@H](C)O)C(=O)CCN(CCCCN)C(=O)CN(CCc1c[nH]c2ccccc12)C(=O)CCN(Cc1ccccc1)C(C)=O 10.1039/C2MD20265D
155541897 179834 0 None -5 2 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 583 7 3 9 3.7 CC(C)CCO[C@@H]1[C@@H](O)[C@@H](O)[C@H]2Cn3cc(nn3)COCCCCCCN(CCc3c[nH]c4ccccc34)CC[C@H]1O2 10.1016/j.ejmech.2018.11.030
CHEMBL4519358 179834 0 None -5 2 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 583 7 3 9 3.7 CC(C)CCO[C@@H]1[C@@H](O)[C@@H](O)[C@H]2Cn3cc(nn3)COCCCCCCN(CCc3c[nH]c4ccccc34)CC[C@H]1O2 10.1016/j.ejmech.2018.11.030
44309052 210726 0 None -109 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human sst4 receptor expressed in CHO-K1 cellsBinding affinity towards human sst4 receptor expressed in CHO-K1 cells
ChEMBL 539 7 4 3 4.7 NC[C@H]1CCC[C@@H](CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm980194h
CHEMBL69303 210726 0 None -109 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human sst4 receptor expressed in CHO-K1 cellsBinding affinity towards human sst4 receptor expressed in CHO-K1 cells
ChEMBL 539 7 4 3 4.7 NC[C@H]1CCC[C@@H](CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm980194h
155557409 181442 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 427 8 2 4 4.8 NCCCn1c(CCc2c[nH]c3ccccc23)nnc1Cc1ccc(Cl)c(Cl)c1 10.1039/C8MD00388B
CHEMBL4558708 181442 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 427 8 2 4 4.8 NCCCn1c(CCc2c[nH]c3ccccc23)nnc1Cc1ccc(Cl)c(Cl)c1 10.1039/C8MD00388B
91809285 132540 0 None -186 6 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1880 34 19 19 5.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](CCCCNC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647686 132540 0 None -186 6 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1880 34 19 19 5.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](CCCCNC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
44308836 109568 0 None -616 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human sst4 receptor expressed in CHO-K1 cellsBinding affinity towards human sst4 receptor expressed in CHO-K1 cells
ChEMBL 539 7 4 3 4.7 NCC1CCCC(CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm980194h
CHEMBL305279 109568 0 None -616 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human sst4 receptor expressed in CHO-K1 cellsBinding affinity towards human sst4 receptor expressed in CHO-K1 cells
ChEMBL 539 7 4 3 4.7 NCC1CCCC(CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm980194h
91809276 132531 0 None -74 6 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1620 27 18 16 4.3 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL3647677 132531 0 None -74 6 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1620 27 18 16 4.3 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
44820563 32807 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 534 11 2 4 5.1 CN(CCCc1cnc[nH]1)C(=S)NCCCN(Cc1ccc(Cl)cc1)c1ccc(Br)cn1 10.1039/c1md00200g
CHEMBL1355048 32807 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 534 11 2 4 5.1 CN(CCCc1cnc[nH]1)C(=S)NCCCN(Cc1ccc(Cl)cc1)c1ccc(Br)cn1 10.1039/c1md00200g
10974426 103702 0 None - 1 Human 6.6 pKi = 6.6 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 680 20 2 9 6.1 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cnccn1 10.1021/jm0205088
CHEMBL266004 103702 0 None - 1 Human 6.6 pKi = 6.6 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 680 20 2 9 6.1 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cnccn1 10.1021/jm0205088
142471840 198622 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 440 10 2 5 4.5 COc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5198961 198622 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 440 10 2 5 4.5 COc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL2372956 217101 0 None -51 4 Human 5.5 pKi = 5.5 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
ChEMBL None None None C[C@@H](C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@H](Cc2ccc(Cl)cc2)C(N)=O)NC1=O)C1CCCS1 10.1021/jm9806289
142471665 198486 0 None 602 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 414 8 2 4 4.4 Fc1ccc2c(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5196971 198486 0 None 602 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 414 8 2 4 4.4 Fc1ccc2c(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
142471655 197204 0 None 562 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1ccc2[nH]cc(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
CHEMBL5178013 197204 0 None 562 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1ccc2[nH]cc(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
142471677 198728 0 None 1621 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 478 9 2 4 5.5 FC(F)(F)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5200786 198728 0 None 1621 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 478 9 2 4 5.5 FC(F)(F)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
91809288 132542 0 None -18 6 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1472 23 17 16 1.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCC[S@@+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3647688 132542 0 None -18 6 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1472 23 17 16 1.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCC[S@@+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
142471769 198564 0 None 301 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 456 10 2 6 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccc(OC)cc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5198142 198564 0 None 301 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 456 10 2 6 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccc(OC)cc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
86293506 125597 0 None 229 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 309 3 2 3 2.4 Cc1cc2ccccc2c(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)n1 10.1021/ml500538a
CHEMBL3421842 125597 0 None 229 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 309 3 2 3 2.4 Cc1cc2ccccc2c(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)n1 10.1021/ml500538a
CHEMBL1791306 215702 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of human somatostatin receptor type 4Inhibition of human somatostatin receptor type 4
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm058184l
142471768 198783 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 435 9 2 5 4.4 N#Cc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5201540 198783 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 435 9 2 5 4.4 N#Cc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
10554930 106968 0 None 1 5 Human 5.5 pKi = 5.5 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
ChEMBL 562 17 3 7 4.9 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)C[C@@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL28824 106968 0 None 1 5 Human 5.5 pKi = 5.5 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
ChEMBL 562 17 3 7 4.9 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)C[C@@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL439136 220606 0 None -9 4 Human 6.5 pKi = 6.5 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL3349599 218207 0 None -1000 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O 10.1021/jm021093t
CHEMBL3349604 218212 0 None -794 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]2C[C@@H](OC(=O)NCCN)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O 10.1021/jm021093t
24936235 128620 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 391 10 5 6 0.6 NCCCCCOC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)CN1CCc1c[nH]c2ccccc12 10.1016/j.ejmech.2018.11.030
CHEMBL3589939 128620 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 391 10 5 6 0.6 NCCCCCOC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)CN1CCc1c[nH]c2ccccc12 10.1016/j.ejmech.2018.11.030
2051 10349 24 None -16595 9 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL None None None None 10.1021/jm980118e
5311430 10349 24 None -16595 9 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL None None None None 10.1021/jm980118e
CHEMBL311695 10349 24 None -16595 9 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL None None None None 10.1021/jm980118e
24936235 128620 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4
ChEMBL 391 10 5 6 0.6 NCCCCCOC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)CN1CCc1c[nH]c2ccccc12 10.1039/C4MD00074A
CHEMBL3589939 128620 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4
ChEMBL 391 10 5 6 0.6 NCCCCCOC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)CN1CCc1c[nH]c2ccccc12 10.1039/C4MD00074A
168280615 197659 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 455 10 2 4 5.6 NCCCCCn1c(CCc2c[nH]c3ccccc23)nnc1Cc1ccc(Cl)c(Cl)c1 10.1039/D1MD00044F
CHEMBL5184884 197659 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 455 10 2 4 5.6 NCCCCCn1c(CCc2c[nH]c3ccccc23)nnc1Cc1ccc(Cl)c(Cl)c1 10.1039/D1MD00044F
CHEMBL437448 220498 0 None -208 5 Human 5.5 pKi = 5.5 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Br)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc(Br)cc2)C(N)=O)NC1=O 10.1021/jm9806289
142471703 198511 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 455 10 2 6 4.4 O=[N+]([O-])c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5197218 198511 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 455 10 2 6 4.4 O=[N+]([O-])c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
11125276 107333 0 None - 1 Human 6.4 pKi = 6.4 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 679 20 2 8 6.7 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cccnc1 10.1021/jm0205088
CHEMBL291474 107333 0 None - 1 Human 6.4 pKi = 6.4 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 679 20 2 8 6.7 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cccnc1 10.1021/jm0205088
142471682 198293 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 4 5.1 Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5193951 198293 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 4 5.1 Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
10166743 130724 0 None -47 5 Human 5.4 pKi = 5.4 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 receptor expressed in CHO cells
ChEMBL 439 6 4 2 6.1 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(Cl)cc1 10.1016/s0960-894x(01)00107-x
CHEMBL362859 130724 0 None -47 5 Human 5.4 pKi = 5.4 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 receptor expressed in CHO cells
ChEMBL 439 6 4 2 6.1 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(Cl)cc1 10.1016/s0960-894x(01)00107-x
142471893 197106 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 516 12 2 5 6.1 c1ccc(COc2cccc(Cc3nnc(CCc4c[nH]c5ccccc45)n3CCCc3c[nH]cn3)c2)cc1 10.1039/D1MD00044F
CHEMBL5176454 197106 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 516 12 2 5 6.1 c1ccc(COc2cccc(Cc3nnc(CCc4c[nH]c5ccccc45)n3CCCc3c[nH]cn3)c2)cc1 10.1039/D1MD00044F
142471814 198941 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 440 10 2 5 4.5 COc1ccccc1Cc1nnc(CCc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5203972 198941 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 440 10 2 5 4.5 COc1ccccc1Cc1nnc(CCc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
44385504 67822 0 None -9 5 Human 5.4 pKi = 5.4 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 receptor expressed in CHO cells
ChEMBL 489 7 4 3 6.4 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(OC(F)(F)F)cc1 10.1016/s0960-894x(01)00107-x
CHEMBL176313 67822 0 None -9 5 Human 5.4 pKi = 5.4 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 receptor expressed in CHO cells
ChEMBL 489 7 4 3 6.4 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(OC(F)(F)F)cc1 10.1016/s0960-894x(01)00107-x
13690207 122160 0 None -2041 5 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1039/C2MD20265D
CHEMBL3350037 122160 0 None -2041 5 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1039/C2MD20265D
86294248 125598 1 None 1023 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 298 3 2 4 1.4 Cn1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc21 10.1021/ml500538a
CHEMBL3421843 125598 1 None 1023 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 298 3 2 4 1.4 Cn1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc21 10.1021/ml500538a
142471737 197083 0 None 77 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 1 5 5.8 Cn1cc(CCc2nnc(Cc3ccc(Cl)c(Cl)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
CHEMBL5176020 197083 0 None 77 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 1 5 5.8 Cn1cc(CCc2nnc(Cc3ccc(Cl)c(Cl)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
10553122 40826 0 None 1 2 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 490 12 2 5 4.9 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccccn1)NCCCn1ccnc1 10.1021/jm980118e
CHEMBL142492 40826 0 None 1 2 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 490 12 2 5 4.9 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccccn1)NCCCn1ccnc1 10.1021/jm980118e
9959684 40721 0 None 2 2 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 566 7 2 4 5.6 S=C(NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)N1CCC(c2c[nH]cn2)CC1 10.1021/jm980118e
CHEMBL142402 40721 0 None 2 2 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 566 7 2 4 5.6 S=C(NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)N1CCC(c2c[nH]cn2)CC1 10.1021/jm980118e
10505242 40616 0 None -1 2 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 489 9 3 4 4.4 NCCC/N=C(\S)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL142321 40616 0 None -1 2 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 489 9 3 4 4.4 NCCC/N=C(\S)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL264028 217382 0 None -24 5 Human 6.4 pKi = 6.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(I)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc(I)cc2)C(N)=O)NC1=O 10.1021/jm9806289
51003591 63529 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to human SSTR4Binding affinity to human SSTR4
ChEMBL 661 19 2 6 7.3 NCCCCCOC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2010.11.088
CHEMBL1643110 63529 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to human SSTR4Binding affinity to human SSTR4
ChEMBL 661 19 2 6 7.3 NCCCCCOC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2010.11.088
51003591 63529 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 661 19 2 6 7.3 NCCCCCOC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1CCc1c[nH]c2ccccc12 10.1016/j.ejmech.2018.11.030
CHEMBL1643110 63529 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 661 19 2 6 7.3 NCCCCCOC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1CCc1c[nH]c2ccccc12 10.1016/j.ejmech.2018.11.030
51003591 63529 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4
ChEMBL 661 19 2 6 7.3 NCCCCCOC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1CCc1c[nH]c2ccccc12 10.1039/C4MD00074A
CHEMBL1643110 63529 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4
ChEMBL 661 19 2 6 7.3 NCCCCCOC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1CCc1c[nH]c2ccccc12 10.1039/C4MD00074A
155546826 180428 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 396 8 2 4 4.1 c1ccc(Cn2c(CCc3c[nH]cn3)nnc2CCc2c[nH]c3ccccc23)cc1 10.1039/C8MD00388B
CHEMBL4534401 180428 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 396 8 2 4 4.1 c1ccc(Cn2c(CCc3c[nH]cn3)nnc2CCc2c[nH]c3ccccc23)cc1 10.1039/C8MD00388B
86292350 125599 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 303 3 2 4 1.8 CC(C)(NC(=O)[C@@H]1[C@H]2CNC[C@H]21)c1noc2c(F)cccc12 10.1021/ml500538a
CHEMBL3421844 125599 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 303 3 2 4 1.8 CC(C)(NC(=O)[C@@H]1[C@H]2CNC[C@H]21)c1noc2c(F)cccc12 10.1021/ml500538a
10602230 40741 0 None 1 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 526 9 3 4 4.6 S=C(NCCc1c[nH]cn1)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL142422 40741 0 None 1 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 526 9 3 4 4.6 S=C(NCCc1c[nH]cn1)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
10578474 40961 0 None 3 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 543 10 2 4 5.1 S=C(NCCCN1CCCC1)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL142613 40961 0 None 3 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 543 10 2 4 5.1 S=C(NCCCN1CCCC1)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
155555535 181220 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 464 8 2 4 5.4 Clc1ccc(Cc2nnc(CCc3c[nH]cn3)n2CCc2c[nH]c3ccccc23)cc1Cl 10.1039/C8MD00388B
CHEMBL4553349 181220 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 464 8 2 4 5.4 Clc1ccc(Cc2nnc(CCc3c[nH]cn3)n2CCc2c[nH]c3ccccc23)cc1Cl 10.1039/C8MD00388B
90665459 116036 0 None 4 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 646 11 3 6 2.9 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CCC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
CHEMBL3218121 116036 0 None 4 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 646 11 3 6 2.9 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CCC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
142471716 198271 0 None 208 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5193686 198271 0 None 208 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471767 199061 0 None 1348 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 4 5.1 Clc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5205904 199061 0 None 1348 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 4 5.1 Clc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL442494 220692 0 None -17 5 Human 8.3 pKi = 8.3 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm0005048
142471772 197957 0 None 870 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 488 9 2 4 5.3 Brc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5189042 197957 0 None 870 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 488 9 2 4 5.3 Brc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL1823873 215811 9 None -18 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human SSTR4 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR4 expressed in CHO-K1 cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2013.11.065
100930865 41565 0 None 91 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 488 12 2 4 4.5 C/S(=N/CCCc1c[nH]cn1)NCCCN(Cc1ccc(Br)cc1)c1ccccn1 10.1021/jm980118e
44362068 41565 0 None 91 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 488 12 2 4 4.5 C/S(=N/CCCc1c[nH]cn1)NCCCN(Cc1ccc(Br)cc1)c1ccccn1 10.1021/jm980118e
CHEMBL143100 41565 0 None 91 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 488 12 2 4 4.5 C/S(=N/CCCc1c[nH]cn1)NCCCN(Cc1ccc(Br)cc1)c1ccccn1 10.1021/jm980118e
10580397 106091 0 None 1 5 Human 6.3 pKi = 6.3 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
ChEMBL 677 20 3 7 6.9 NCCCCCNC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL282129 106091 0 None 1 5 Human 6.3 pKi = 6.3 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
ChEMBL 677 20 3 7 6.9 NCCCCCNC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL3349602 218210 0 None -1258 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](OC(=O)NCCN)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O 10.1021/jm021093t
10094509 137464 0 None -138 5 Human 5.3 pKi = 5.3 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 receptor expressed in CHO cells
ChEMBL 435 7 4 3 5.5 COc1ccc(C(=N)N[C@H](Cc2c[nH]c3ccccc23)c2nc(-c3ccccc3)c[nH]2)cc1 10.1016/s0960-894x(01)00107-x
CHEMBL368334 137464 0 None -138 5 Human 5.3 pKi = 5.3 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 receptor expressed in CHO cells
ChEMBL 435 7 4 3 5.5 COc1ccc(C(=N)N[C@H](Cc2c[nH]c3ccccc23)c2nc(-c3ccccc3)c[nH]2)cc1 10.1016/s0960-894x(01)00107-x
142471828 198851 0 None 134 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 478 9 2 4 5.8 Clc1cc(Cl)cc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5202717 198851 0 None 134 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 478 9 2 4 5.8 Clc1cc(Cl)cc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
10769191 40566 0 None 3 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 557 11 2 4 5.5 S=C(NCCCN1CCCC1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL142283 40566 0 None 3 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 557 11 2 4 5.5 S=C(NCCCN1CCCC1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
10841338 40881 0 None 3 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 602 10 3 4 7.3 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)Nc1cccc(-c2c[nH]cn2)c1 10.1021/jm980118e
CHEMBL142549 40881 0 None 3 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 602 10 3 4 7.3 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)Nc1cccc(-c2c[nH]cn2)c1 10.1021/jm980118e
10531093 175043 0 None 10 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 568 12 3 4 5.8 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCCc1c[nH]cn1 10.1021/jm980118e
CHEMBL433872 175043 0 None 10 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 568 12 3 4 5.8 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCCc1c[nH]cn1 10.1021/jm980118e
11828523 201784 0 None - 1 Human 7.3 pKi = 7.3 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 669 20 3 9 5.5 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2cnc[nH]2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cccnc1 10.1021/jm0205088
CHEMBL54832 201784 0 None - 1 Human 7.3 pKi = 7.3 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 669 20 3 9 5.5 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2cnc[nH]2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cccnc1 10.1021/jm0205088
155565048 182280 0 None -1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 484 10 1 8 3.3 CC(=O)O[C@H]1CN(Cc2cccc3ccccc23)[C@H](CCCCCN)[C@@H](OC(C)=O)[C@@H]1OC(C)=O 10.1016/j.ejmech.2018.11.030
CHEMBL4577766 182280 0 None -1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 484 10 1 8 3.3 CC(=O)O[C@H]1CN(Cc2cccc3ccccc23)[C@H](CCCCCN)[C@@H](OC(C)=O)[C@@H]1OC(C)=O 10.1016/j.ejmech.2018.11.030
122181226 128623 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4
ChEMBL 484 10 1 8 3.3 CC(=O)O[C@H]1CN(Cc2ccc3ccccc3c2)[C@H](CCCCCN)[C@@H](OC(C)=O)[C@@H]1OC(C)=O 10.1039/C4MD00074A
CHEMBL3589941 128623 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4
ChEMBL 484 10 1 8 3.3 CC(=O)O[C@H]1CN(Cc2ccc3ccccc3c2)[C@H](CCCCCN)[C@@H](OC(C)=O)[C@@H]1OC(C)=O 10.1039/C4MD00074A
142471733 197344 0 None 75 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 394 7 2 4 4.4 CC(C)(C)Cc1nnc(Cc2c[nH]c3cc(F)ccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5180116 197344 0 None 75 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 394 7 2 4 4.4 CC(C)(C)Cc1nnc(Cc2c[nH]c3cc(F)ccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
11050695 202263 0 None - 1 Human 6.2 pKi = 6.2 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 679 20 2 8 6.7 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccncc1 10.1021/jm0205088
CHEMBL55298 202263 0 None - 1 Human 6.2 pKi = 6.2 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 679 20 2 8 6.7 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccncc1 10.1021/jm0205088
CHEMBL2369734 216441 0 None -8 5 Human 6.2 pKi = 6.2 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)N(C)C1=O 10.1021/jm0005048
168295000 199251 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 474 9 2 6 3.7 CS(=O)(=O)c1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5208764 199251 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 474 9 2 6 3.7 CS(=O)(=O)c1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
56651207 182676 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 655 10 5 9 3.6 NC/C=C/CO[C@@H]1[C@@H](NC(=O)Cc2c[nH]c3ccccc23)COC(=O)c2c(O)cccc2/C=C/COC[C@@H](OCc2ccccc2)[C@H]1O 10.1016/j.ejmech.2018.11.030
CHEMBL4586779 182676 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 655 10 5 9 3.6 NC/C=C/CO[C@@H]1[C@@H](NC(=O)Cc2c[nH]c3ccccc23)COC(=O)c2c(O)cccc2/C=C/COC[C@@H](OCc2ccccc2)[C@H]1O 10.1016/j.ejmech.2018.11.030
44385712 67118 0 None -8 4 Human 5.2 pKi = 5.2 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 receptor expressed in CHO cells
ChEMBL 343 5 4 2 4.4 CC(=N)N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1 10.1016/s0960-894x(01)00107-x
CHEMBL174490 67118 0 None -8 4 Human 5.2 pKi = 5.2 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 receptor expressed in CHO cells
ChEMBL 343 5 4 2 4.4 CC(=N)N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1 10.1016/s0960-894x(01)00107-x
90644981 118590 0 None -660 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]SS14 from human SST4 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST4 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 365 5 3 2 4.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287613 118590 0 None -660 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]SS14 from human SST4 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST4 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 365 5 3 2 4.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
9893924 11520 34 None 52 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in BHK cell membranes after 30 to 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in BHK cell membranes after 30 to 90 mins by gamma counting method
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1039/C8MD00388B
CHEMBL103769 11520 34 None 52 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in BHK cell membranes after 30 to 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in BHK cell membranes after 30 to 90 mins by gamma counting method
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1039/C8MD00388B
9893924 11520 34 None 52 2 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL103769 11520 34 None 52 2 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
9893924 11520 34 None 52 2 Human 8.2 pKi = 8.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm0108449
CHEMBL103769 11520 34 None 52 2 Human 8.2 pKi = 8.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm0108449
168283525 197866 0 None 851 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 439 8 2 5 4.3 N#Cc1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5187631 197866 0 None 851 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 439 8 2 5 4.3 N#Cc1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL1791304 215700 0 None -25 2 Human 7.2 pKi = 7.2 Binding
Inhibition of human somatostatin receptor type 4Inhibition of human somatostatin receptor type 4
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnccn2)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm058184l
91809284 132539 0 None -288 6 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1896 34 20 20 5.5 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](CCCCNC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3647685 132539 0 None -288 6 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1896 34 20 20 5.5 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](CCCCNC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
91809277 132532 0 None -204 6 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1457 23 16 14 3.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL3647678 132532 0 None -204 6 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1457 23 16 14 3.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL3349603 218211 0 None -999 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None NCCCCCNC(=O)O[C@@H]1C[C@H]2C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc3ccc(OCc4ccccc4)cc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N2C1 10.1021/jm021093t
168283125 197856 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 441 9 2 4 5.2 NCCCCn1c(CCc2c[nH]c3ccccc23)nnc1Cc1ccc(Cl)c(Cl)c1 10.1039/D1MD00044F
CHEMBL5187484 197856 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 441 9 2 4 5.2 NCCCCn1c(CCc2c[nH]c3ccccc23)nnc1Cc1ccc(Cl)c(Cl)c1 10.1039/D1MD00044F
2055 9682 48 None -501 14 Human 7.2 pKi = 7.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL None None None None 10.1039/C8MD00388B
383414 9682 48 None -501 14 Human 7.2 pKi = 7.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL None None None None 10.1039/C8MD00388B
448601 9682 48 None -501 14 Human 7.2 pKi = 7.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL None None None None 10.1039/C8MD00388B
90488715 9682 48 None -501 14 Human 7.2 pKi = 7.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL None None None None 10.1039/C8MD00388B
CHEMBL1680 9682 48 None -501 14 Human 7.2 pKi = 7.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL None None None None 10.1039/C8MD00388B
CHEMBL262746 9682 48 None -501 14 Human 7.2 pKi = 7.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL None None None None 10.1039/C8MD00388B
DB00104 9682 48 None -501 14 Human 7.2 pKi = 7.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL None None None None 10.1039/C8MD00388B
44386389 136861 0 None -13 5 Human 5.2 pKi = 5.2 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 receptor expressed in CHO cells
ChEMBL 473 6 4 2 6.5 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(C(F)(F)F)cc1 10.1016/s0960-894x(01)00107-x
CHEMBL367699 136861 0 None -13 5 Human 5.2 pKi = 5.2 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 receptor expressed in CHO cells
ChEMBL 473 6 4 2 6.5 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(C(F)(F)F)cc1 10.1016/s0960-894x(01)00107-x
CHEMBL406738 219397 0 None -8 5 Human 6.2 pKi = 6.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
ChEMBL None None None CC(C)CC[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
10887003 201492 0 None - 1 Human 6.2 pKi = 6.2 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 697 20 2 8 6.9 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccc(F)nc1 10.1021/jm0205088
CHEMBL53440 201492 0 None - 1 Human 6.2 pKi = 6.2 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 697 20 2 8 6.9 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccc(F)nc1 10.1021/jm0205088
155528330 178119 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 513 11 5 7 2.5 Cc1ccc(S[C@H]2O[C@H](CO)[C@@H](O)[C@H](OCCCCN)[C@@H]2NC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.ejmech.2018.11.030
CHEMBL4461404 178119 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 513 11 5 7 2.5 Cc1ccc(S[C@H]2O[C@H](CO)[C@@H](O)[C@H](OCCCCN)[C@@H]2NC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.ejmech.2018.11.030
CHEMBL2372959 217104 0 None -2 5 Human 6.2 pKi = 6.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H](N)C2Cc3ccccc3C2)CSSC[C@@H](C(=O)N[C@H](C(N)=O)C2Cc3ccccc3C2)NC1=O 10.1021/jm9806289
9827283 85363 0 None -147 4 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human sst4 receptor expressed in CHO-K1 cellsBinding affinity towards human sst4 receptor expressed in CHO-K1 cells
ChEMBL 499 9 4 3 4.1 NCCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/jm980194h
CHEMBL2112223 85363 0 None -147 4 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human sst4 receptor expressed in CHO-K1 cellsBinding affinity towards human sst4 receptor expressed in CHO-K1 cells
ChEMBL 499 9 4 3 4.1 NCCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/jm980194h
44820544 59178 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 396 9 4 4 2.5 S=C(NCCCNc1ccc(Br)cn1)NCCCc1c[nH]cn1 10.1039/c1md00200g
CHEMBL1590268 59178 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 396 9 4 4 2.5 S=C(NCCCNc1ccc(Br)cn1)NCCCc1c[nH]cn1 10.1039/c1md00200g
142471923 198690 0 None 512 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 488 10 2 6 3.9 CS(=O)(=O)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5200112 198690 0 None 512 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 488 10 2 6 3.9 CS(=O)(=O)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
168271446 197384 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 421 8 2 5 4.2 N#Cc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5180752 197384 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 421 8 2 5 4.2 N#Cc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
91809303 132556 0 None -22 6 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1659 28 18 16 3.8 CC(=O)N(CCC(=O)N[C@@H](CN[C@@H]1CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O)Cc1ccc(O)cc1)C[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 nan
CHEMBL3647702 132556 0 None -22 6 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1659 28 18 16 3.8 CC(=O)N(CCC(=O)N[C@@H](CN[C@@H]1CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O)Cc1ccc(O)cc1)C[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 nan
142471692 199161 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 440 10 2 5 4.5 COc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5207543 199161 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 440 10 2 5 4.5 COc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
10554498 38063 0 None 4 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 540 10 3 4 5.0 S=C(NCCCc1c[nH]cn1)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL140151 38063 0 None 4 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 540 10 3 4 5.0 S=C(NCCCc1c[nH]cn1)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
117711399 125600 0 None 104 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 310 3 2 4 1.8 Cc1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc2n1 10.1021/ml500538a
CHEMBL3421845 125600 0 None 104 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 310 3 2 4 1.8 Cc1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc2n1 10.1021/ml500538a
CHEMBL1791305 215701 0 None - 1 Human 6.2 pKi = 6.2 Binding
Inhibition of human somatostatin receptor type 4Inhibition of human somatostatin receptor type 4
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2cnccn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm058184l
10528970 41206 0 None 4 2 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 486 11 2 5 4.0 S=C(NCCCN(Cc1ccc(Br)cc1)c1ccccn1)NCCCn1ccnc1 10.1021/jm980118e
CHEMBL142822 41206 0 None 4 2 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 486 11 2 5 4.0 S=C(NCCCN(Cc1ccc(Br)cc1)c1ccccn1)NCCCn1ccnc1 10.1021/jm980118e
10720221 41863 0 None 1 2 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 500 12 2 5 4.4 S=C(NCCCCN(Cc1ccc(Br)cc1)c1ccccn1)NCCCn1ccnc1 10.1021/jm980118e
CHEMBL143367 41863 0 None 1 2 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 500 12 2 5 4.4 S=C(NCCCCN(Cc1ccc(Br)cc1)c1ccccn1)NCCCn1ccnc1 10.1021/jm980118e
127032865 145539 0 None -1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting methodDisplacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting method
ChEMBL 393 6 1 3 5.4 NCCCc1cc(Cl)cc2c1OC(CCc1cccc3ccccc13)CC2=O 10.1016/j.ejmech.2016.02.046
CHEMBL3780496 145539 0 None -1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting methodDisplacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting method
ChEMBL 393 6 1 3 5.4 NCCCc1cc(Cl)cc2c1OC(CCc1cccc3ccccc13)CC2=O 10.1016/j.ejmech.2016.02.046
44385652 67166 0 None -28 5 Human 5.2 pKi = 5.2 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 receptor expressed in CHO cells
ChEMBL 405 6 4 2 5.5 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccccc1 10.1016/s0960-894x(01)00107-x
CHEMBL174872 67166 0 None -28 5 Human 5.2 pKi = 5.2 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 receptor expressed in CHO cells
ChEMBL 405 6 4 2 5.5 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccccc1 10.1016/s0960-894x(01)00107-x
2070 7484 5 None -11220 4 Human 5.2 pKi = 5.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/jm0108449
9802572 7484 5 None -11220 4 Human 5.2 pKi = 5.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/jm0108449
CHEMBL2069499 7484 5 None -11220 4 Human 5.2 pKi = 5.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/jm0108449
44361984 41193 0 None - 1 Human 4.2 pKi = 4.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 510 12 2 3 5.7 S=C(NCCCCN(Cc1ccc(Br)cc1)c1ccccn1)NCCCc1ccccc1 10.1021/jm980118e
CHEMBL142811 41193 0 None - 1 Human 4.2 pKi = 4.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 510 12 2 3 5.7 S=C(NCCCCN(Cc1ccc(Br)cc1)c1ccccn1)NCCCc1ccccc1 10.1021/jm980118e
10793795 41993 0 None - 1 Human 4.2 pKi = 4.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 605 9 2 4 7.5 S=C(NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)Nc1ccc(N2CCCCC2)cc1 10.1021/jm980118e
CHEMBL143539 41993 0 None - 1 Human 4.2 pKi = 4.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 605 9 2 4 7.5 S=C(NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)Nc1ccc(N2CCCCC2)cc1 10.1021/jm980118e
168286554 198182 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 324 6 2 4 2.8 Fc1ccc2c(Cc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5192578 198182 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 324 6 2 4 2.8 Fc1ccc2c(Cc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
90665460 116037 0 None -3 5 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 793 13 3 7 3.9 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
CHEMBL3218122 116037 0 None -3 5 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 793 13 3 7 3.9 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
155529288 178176 0 None 1 2 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 1072 19 12 13 0.7 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)C(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2018.11.030
CHEMBL4462329 178176 0 None 1 2 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 1072 19 12 13 0.7 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)C(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2018.11.030
44377555 64305 0 None -12 5 Human 5.1 pKi = 5.1 Binding
Inhibitory constant on human somatostatin receptor 4Inhibitory constant on human somatostatin receptor 4
ChEMBL 384 5 1 5 5.2 NCCCc1nc(-c2csc3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
CHEMBL166247 64305 0 None -12 5 Human 5.1 pKi = 5.1 Binding
Inhibitory constant on human somatostatin receptor 4Inhibitory constant on human somatostatin receptor 4
ChEMBL 384 5 1 5 5.2 NCCCc1nc(-c2csc3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
71458043 85678 0 None -6 5 Human 5.1 pKi = 5.1 Binding
Inhibitory constant on human somatostatin receptor 4Inhibitory constant on human somatostatin receptor 4
ChEMBL 494 10 3 5 4.3 CC(C)(C(=O)NCCc1c[nH]c2ccccc12)c1cn2cc(Cc3ccccc3)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
CHEMBL2112934 85678 0 None -6 5 Human 5.1 pKi = 5.1 Binding
Inhibitory constant on human somatostatin receptor 4Inhibitory constant on human somatostatin receptor 4
ChEMBL 494 10 3 5 4.3 CC(C)(C(=O)NCCc1c[nH]c2ccccc12)c1cn2cc(Cc3ccccc3)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
CHEMBL410181 219584 0 None -2 5 Human 6.1 pKi = 6.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
44397389 130822 0 None -43 5 Human 7.1 pKi = 7.1 Binding
Binding affinity against human sst4 receptor at a dose of 10 uMBinding affinity against human sst4 receptor at a dose of 10 uM
ChEMBL 460 9 2 6 5.2 NCCCCn1c(SCCc2c[nH]c3cc(F)ccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL363092 130822 0 None -43 5 Human 7.1 pKi = 7.1 Binding
Binding affinity against human sst4 receptor at a dose of 10 uMBinding affinity against human sst4 receptor at a dose of 10 uM
ChEMBL 460 9 2 6 5.2 NCCCCn1c(SCCc2c[nH]c3cc(F)ccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL1791304 215700 0 None -25 2 Human 7.1 pKi = 7.1 Binding
Inhibition of human somatostatin receptor type 4 (n=5)Inhibition of human somatostatin receptor type 4 (n=5)
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnccn2)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm058184l
CHEMBL2369719 216436 0 None -3 2 Human 7.1 pKi = 7.1 Binding
Inhibition of human somatostatin receptor type 4Inhibition of human somatostatin receptor type 4
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm058184l
168297256 199190 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 2 6 3.8 CS(=O)(=O)c1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5208037 199190 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 2 6 3.8 CS(=O)(=O)c1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
11705763 175094 0 None -2089 5 Human 6.1 pKi = 6.1 Binding
Binding affinity against human sst4 receptor at a dose of 10 uMBinding affinity against human sst4 receptor at a dose of 10 uM
ChEMBL 484 10 2 7 5.4 Cc1cccc2c(C(=O)CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
CHEMBL434159 175094 0 None -2089 5 Human 6.1 pKi = 6.1 Binding
Binding affinity against human sst4 receptor at a dose of 10 uMBinding affinity against human sst4 receptor at a dose of 10 uM
ChEMBL 484 10 2 7 5.4 Cc1cccc2c(C(=O)CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
10768264 41627 0 None 2 2 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 517 10 2 4 5.0 CN(C)CCC/N=C(\S)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL143164 41627 0 None 2 2 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 517 10 2 4 5.0 CN(C)CCC/N=C(\S)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
15965425 8987 7 None -8128 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human somatostatin receptor type 4Binding affinity to human somatostatin receptor type 4
ChEMBL 645 11 5 7 4.3 NCCCC[C@@H](C(=O)OC(C)(C)C)NC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01029
2046 8987 7 None -8128 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human somatostatin receptor type 4Binding affinity to human somatostatin receptor type 4
ChEMBL 645 11 5 7 4.3 NCCCC[C@@H](C(=O)OC(C)(C)C)NC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01029
CHEMBL99895 8987 7 None -8128 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human somatostatin receptor type 4Binding affinity to human somatostatin receptor type 4
ChEMBL 645 11 5 7 4.3 NCCCC[C@@H](C(=O)OC(C)(C)C)NC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01029
15965425 8987 7 None -8128 5 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Somatostatin receptor type 4 (hsst4)Binding affinity towards Somatostatin receptor type 4 (hsst4)
ChEMBL 645 11 5 7 4.3 NCCCC[C@@H](C(=O)OC(C)(C)C)NC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm020424z
2046 8987 7 None -8128 5 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Somatostatin receptor type 4 (hsst4)Binding affinity towards Somatostatin receptor type 4 (hsst4)
ChEMBL 645 11 5 7 4.3 NCCCC[C@@H](C(=O)OC(C)(C)C)NC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm020424z
CHEMBL99895 8987 7 None -8128 5 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Somatostatin receptor type 4 (hsst4)Binding affinity towards Somatostatin receptor type 4 (hsst4)
ChEMBL 645 11 5 7 4.3 NCCCC[C@@H](C(=O)OC(C)(C)C)NC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm020424z
168274078 197067 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 320 7 2 4 2.9 c1ccc2c(CCc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5175762 197067 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 320 7 2 4 2.9 c1ccc2c(CCc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
44363816 46449 0 None -22 5 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 4 (hSSTR-4)In vitro binding affinity was evaluated against human Somatostatin receptor type 4 (hSSTR-4)
ChEMBL 589 14 3 5 5.0 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(CCCc2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL147499 46449 0 None -22 5 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 4 (hSSTR-4)In vitro binding affinity was evaluated against human Somatostatin receptor type 4 (hSSTR-4)
ChEMBL 589 14 3 5 5.0 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(CCCc2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL407496 219444 0 None -27 5 Human 6.1 pKi = 6.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(F)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL2372964 217109 0 None -6 4 Human 6.1 pKi = 6.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
ChEMBL None None None C[C@@H](C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(F)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O)C1CCCS1 10.1021/jm9806289
10963480 107544 0 None - 1 Human 6.1 pKi = 6.1 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 679 20 2 8 6.7 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccn1 10.1021/jm0205088
CHEMBL292906 107544 0 None - 1 Human 6.1 pKi = 6.1 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 679 20 2 8 6.7 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccn1 10.1021/jm0205088
CHEMBL2372961 217106 0 None -74 4 Human 6.1 pKi = 6.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
ChEMBL None None None C[C@@H](C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O)C1CCCS1 10.1021/jm9806289
91809275 132530 0 None -776 6 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1603 27 18 17 3.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647676 132530 0 None -776 6 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1603 27 18 17 3.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
142471746 197493 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 486 10 2 4 6.2 c1ccc(-c2ccc(Cc3nnc(CCc4c[nH]c5ccccc45)n3CCCc3c[nH]cn3)cc2)cc1 10.1039/D1MD00044F
CHEMBL5182380 197493 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 486 10 2 4 6.2 c1ccc(-c2ccc(Cc3nnc(CCc4c[nH]c5ccccc45)n3CCCc3c[nH]cn3)cc2)cc1 10.1039/D1MD00044F
11800917 41887 0 None 20 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 554 11 3 4 5.4 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCc1c[nH]cn1 10.1021/jm980118e
CHEMBL143409 41887 0 None 20 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 554 11 3 4 5.4 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCc1c[nH]cn1 10.1021/jm980118e
11112736 23301 0 None -8128 3 Human 5.0 pKi = 5.0 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL1237140 23301 0 None -8128 3 Human 5.0 pKi = 5.0 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL1788167 23301 0 None -8128 3 Human 5.0 pKi = 5.0 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL2370166 216584 0 None -120 5 Human 6.0 pKi = 6.0 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in CHO-K1 cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in CHO-K1 cells.
ChEMBL None None None C[C@@H](c1ccccc1)N1CC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCNC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C1=O 10.1021/jm970393l
168271928 196862 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 306 6 2 4 2.7 c1ccc2c(Cc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5172730 196862 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 306 6 2 4 2.7 c1ccc2c(Cc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
2078 7408 0 None -1 2 Mouse 7.4 pKd = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12595949
73755026 7408 0 None -1 2 Mouse 7.4 pKd = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12595949
2078 7408 0 None 1 2 Human 7.6 pKd = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12595949
73755026 7408 0 None 1 2 Human 7.6 pKd = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12595949
2055 9682 48 125I-Tyr11-SRIF 1 14 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-Tyr11-SRIF 1 14 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
448601 9682 48 125I-Tyr11-SRIF 1 14 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-Tyr11-SRIF 1 14 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-Tyr11-SRIF 1 14 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-Tyr11-SRIF 1 14 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-Tyr11-SRIF 1 14 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 125I-Tyr11-SRIF -501 14 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-Tyr11-SRIF -501 14 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
448601 9682 48 125I-Tyr11-SRIF -501 14 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-Tyr11-SRIF -501 14 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-Tyr11-SRIF -501 14 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-Tyr11-SRIF -501 14 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-Tyr11-SRIF -501 14 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 222875 0 125I-Tyr11-somatostatin-14 -9 13 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
None 223128 0 Functional 537 5 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 485 11 4 4 3.1 COC(=O)C(CCCN=C(N)N)NC(=O)CCCC1=C(NC2=C(C=C(C=C12)F)F)C3=CC=CC=C3 None
16161315 222875 0 UNDEFINED -9 13 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-LTT-SST-28 -9 13 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
2055 9682 48 125I-CGP23996 1 14 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-CGP23996 1 14 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
448601 9682 48 125I-CGP23996 1 14 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-CGP23996 1 14 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-CGP23996 1 14 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-CGP23996 1 14 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-CGP23996 1 14 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 222875 0 125I-Tyr11-SRIF-14 -9 13 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
None 223128 0 125I-LTT-SST-28 537 5 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 485 11 4 4 3.1 COC(=O)C(CCCN=C(N)N)NC(=O)CCCC1=C(NC2=C(C=C(C=C12)F)F)C3=CC=CC=C3 None
None 223128 0 UNDEFINED 537 5 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 485 11 4 4 3.1 COC(=O)C(CCCN=C(N)N)NC(=O)CCCC1=C(NC2=C(C=C(C=C12)F)F)C3=CC=CC=C3 None
16161315 222875 0 125I-CGP23996 -18 13 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-Tyr11-somatostatin -18 13 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-LTT-SST-28 -9 13 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-Tyr11-SRIF -9 13 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-Tyr11-SRIF -9 13 Mouse 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-LTT-SRIF28 -9 13 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-SRIF-28 -9 13 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-SOMATOSTATIN 14 -9 13 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-SRIF -9 13 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-CGP23996 -9 13 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
2055 9682 48 125I-LTT-SST-28 -501 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-LTT-SST-28 -501 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
448601 9682 48 125I-LTT-SST-28 -501 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-LTT-SST-28 -501 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-LTT-SST-28 -501 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-LTT-SST-28 -501 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-LTT-SST-28 -501 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 222875 0 125I-Tyr11-SRIF -9 13 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-LTT-SST-28 -9 13 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-LTT-SST-28 -9 13 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-SOMATOSTATIN -9 13 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-Tyr11-somatostatin-14 -9 13 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
2055 9682 48 125I-LTT-SST-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 125I-SOMATOSTATIN -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 125I-SOMATOSTATIN 14 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 125I-SRIF -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 125I-SRIF-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 UNDEFINED -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 125I-Tyr11-SRIF -3090 14 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-LTT-SST-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-SOMATOSTATIN -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-SOMATOSTATIN 14 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-SRIF -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-SRIF-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 UNDEFINED -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-Tyr11-SRIF -3090 14 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
448601 9682 48 125I-LTT-SST-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
448601 9682 48 125I-SOMATOSTATIN -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
448601 9682 48 125I-SOMATOSTATIN 14 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
448601 9682 48 125I-SRIF -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
448601 9682 48 125I-SRIF-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
448601 9682 48 UNDEFINED -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
448601 9682 48 125I-Tyr11-SRIF -3090 14 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-LTT-SST-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-SOMATOSTATIN -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-SOMATOSTATIN 14 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-SRIF -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-SRIF-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 UNDEFINED -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-Tyr11-SRIF -3090 14 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-LTT-SST-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-SOMATOSTATIN -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-SOMATOSTATIN 14 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-SRIF -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-SRIF-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 UNDEFINED -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-Tyr11-SRIF -3090 14 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-LTT-SST-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-SOMATOSTATIN -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-SOMATOSTATIN 14 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-SRIF -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-SRIF-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 UNDEFINED -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-Tyr11-SRIF -3090 14 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-LTT-SST-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-SOMATOSTATIN -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-SOMATOSTATIN 14 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-SRIF -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-SRIF-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 UNDEFINED -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-Tyr11-SRIF -3090 14 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
None 222876 0 125I-SOMATOSTATIN -1288 12 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 222876 0 125I-SRIF -1288 12 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 222876 0 125I-SRIF-28 -1288 12 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 222876 0 125I-Tyr11-SRIF -6025 12 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
2247 7293 81 UNDEFINED -5754 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 7293 81 UNDEFINED -5754 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 7293 81 UNDEFINED -5754 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 7293 81 UNDEFINED -5754 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 7293 81 UNDEFINED -5754 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
46882665 12404 0 UNDEFINED -15 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 382 7 1 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cccnc4o3)CC2)ccc1OC None
CHEMBL1077721 12404 0 UNDEFINED -15 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 382 7 1 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cccnc4o3)CC2)ccc1OC None
46882666 12405 0 UNDEFINED -13 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 382 7 1 7 3.7 CCOc1cc(CN2CCC(Nc3nc4ccncc4o3)CC2)ccc1OC None
CHEMBL1077722 12405 0 UNDEFINED -13 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 382 7 1 7 3.7 CCOc1cc(CN2CCC(Nc3nc4ccncc4o3)CC2)ccc1OC None
46882746 12409 0 UNDEFINED -21 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 1 6 3.9 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OC None
CHEMBL1077742 12409 0 UNDEFINED -21 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 1 6 3.9 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OC None
24740861 12450 0 UNDEFINED -20 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 399 8 1 6 4.3 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCCF None
CHEMBL1077877 12450 0 UNDEFINED -20 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 399 8 1 6 4.3 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCCF None
46882789 12451 0 UNDEFINED -19 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 419 6 1 5 5.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1C(F)(F)F None
CHEMBL1077887 12451 0 UNDEFINED -19 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 419 6 1 5 5.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1C(F)(F)F None
46882181 12453 0 UNDEFINED -50 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 536 10 2 8 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5ccccc5)ccc4o3)CC2)ccc1OC None
CHEMBL1077908 12453 0 UNDEFINED -50 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 536 10 2 8 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5ccccc5)ccc4o3)CC2)ccc1OC None
46882790 12474 0 UNDEFINED -18 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 407 8 1 6 4.8 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC1CC1 None
CHEMBL1078081 12474 0 UNDEFINED -18 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 407 8 1 6 4.8 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC1CC1 None
46882620 12487 0 UNDEFINED -28 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 465 8 1 7 5.2 CCOc1cc(CN2CCC(Nc3nc4cc(OC(F)(F)F)ccc4o3)CC2)ccc1OC None
CHEMBL1078215 12487 0 UNDEFINED -28 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 465 8 1 7 5.2 CCOc1cc(CN2CCC(Nc3nc4cc(OC(F)(F)F)ccc4o3)CC2)ccc1OC None
46882664 12489 0 UNDEFINED -28 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 494 8 2 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1OC None
CHEMBL1078240 12489 0 UNDEFINED -28 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 494 8 2 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1OC None
46882621 12495 0 UNDEFINED -28 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 438 8 2 7 4.3 CCOc1cc(CN2CCC(Nc3nc4cc(NC(C)=O)ccc4o3)CC2)ccc1OC None
CHEMBL1078283 12495 0 UNDEFINED -28 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 438 8 2 7 4.3 CCOc1cc(CN2CCC(Nc3nc4cc(NC(C)=O)ccc4o3)CC2)ccc1OC None
46882831 12516 0 UNDEFINED -301 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 8 2 7 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OCC)c1N None
CHEMBL1078449 12516 0 UNDEFINED -301 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 8 2 7 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OCC)c1N None
46882832 12518 0 UNDEFINED -64 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 467 10 1 8 4.9 CCOC(=O)c1c(OCC)cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCC None
CHEMBL1078450 12518 0 UNDEFINED -64 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 467 10 1 8 4.9 CCOC(=O)c1c(OCC)cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCC None
11848626 12519 0 UNDEFINED -56 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 413 8 1 6 4.8 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OCC)c1F None
CHEMBL1078451 12519 0 UNDEFINED -56 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 413 8 1 6 4.8 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OCC)c1F None
46882622 12534 0 UNDEFINED -44 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 488 9 1 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)ccc1OC None
CHEMBL1078528 12534 0 UNDEFINED -44 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 488 9 1 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)ccc1OC None
11848625 12564 0 UNDEFINED -107 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 None
CHEMBL1078745 12564 0 UNDEFINED -107 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 None
46882708 12575 0 UNDEFINED -26 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 380 7 2 6 4.3 CCNc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
CHEMBL1078841 12575 0 UNDEFINED -26 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 380 7 2 6 4.3 CCNc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
11848833 12579 0 UNDEFINED -323 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 423 8 1 6 5.5 CC(C)Oc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC(C)C)c1 None
CHEMBL1078895 12579 0 UNDEFINED -323 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 423 8 1 6 5.5 CC(C)Oc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC(C)C)c1 None
46882133 12580 0 UNDEFINED -54 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 478 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NC(=O)C5CCC5)ccc4o3)CC2)ccc1OC None
CHEMBL1078896 12580 0 UNDEFINED -54 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 478 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NC(=O)C5CCC5)ccc4o3)CC2)ccc1OC None
46882445 12583 0 UNDEFINED -30 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 6 1 6 4.8 CCOc1cc(N2CCC(Nc3nc4ccccc4s3)CC2)ccc1OC None
CHEMBL1078903 12583 0 UNDEFINED -30 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 6 1 6 4.8 CCOc1cc(N2CCC(Nc3nc4ccccc4s3)CC2)ccc1OC None
46882180 12613 0 UNDEFINED -39 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 482 7 2 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1F None
CHEMBL1079180 12613 0 UNDEFINED -39 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 482 7 2 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1F None
46882577 12629 1 UNDEFINED -51 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 415 7 1 6 5.0 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)ccc4o3)CC2)ccc1OC None
CHEMBL1079312 12629 1 UNDEFINED -51 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 415 7 1 6 5.0 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)ccc4o3)CC2)ccc1OC None
46882578 12630 0 UNDEFINED -51 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 473 9 1 8 4.1 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)ccc1OC None
CHEMBL1079313 12630 0 UNDEFINED -51 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 473 9 1 8 4.1 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)ccc1OC None
46882579 12631 0 UNDEFINED -39 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 1 8 4.2 CCOc1cc(CN2CCC(Nc3nc4cc([N+](=O)[O-])ccc4o3)CC2)ccc1OC None
CHEMBL1079314 12631 0 UNDEFINED -39 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 1 8 4.2 CCOc1cc(CN2CCC(Nc3nc4cc([N+](=O)[O-])ccc4o3)CC2)ccc1OC None
46882182 12693 0 UNDEFINED -190 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 567 11 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)cc(OCC)c1-n1cccc1 None
CHEMBL1079686 12693 0 UNDEFINED -190 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 567 11 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)cc(OCC)c1-n1cccc1 None
16062555 12728 0 UNDEFINED -562 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 457 9 2 7 4.5 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)cc(OCC)c1F None
CHEMBL1079874 12728 0 UNDEFINED -562 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 457 9 2 7 4.5 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)cc(OCC)c1F None
11848835 12835 0 UNDEFINED -1258 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 456 9 2 7 3.9 CCOc1cc(CN2CCC(Nc3nc4cc(C(N)=O)ccc4o3)CC2)cc(OCC)c1F None
CHEMBL1080584 12835 0 UNDEFINED -1258 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 456 9 2 7 3.9 CCOc1cc(CN2CCC(Nc3nc4cc(C(N)=O)ccc4o3)CC2)cc(OCC)c1F None
16062816 12836 0 UNDEFINED -3311 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 473 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(C(=O)O)ccc4o3)CC2)cc(OCC)c1Cl None
CHEMBL1080585 12836 0 UNDEFINED -3311 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 473 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(C(=O)O)ccc4o3)CC2)cc(OCC)c1Cl None
16062553 12837 0 UNDEFINED -436 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 429 7 2 6 4.7 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)ccc1Cl None
CHEMBL1080586 12837 0 UNDEFINED -436 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 429 7 2 6 4.7 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)ccc1Cl None
46882225 12919 0 UNDEFINED -39 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 526 9 2 8 4.1 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)cc(OCC)c1F None
CHEMBL1080950 12919 0 UNDEFINED -39 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 526 9 2 8 4.1 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)cc(OCC)c1F None
46882226 12920 0 UNDEFINED -41 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 419 6 1 5 5.6 CCOc1cc(CN2CCC(Nc3nc4ccc(Cl)cc4o3)CC2)ccc1Cl None
CHEMBL1080951 12920 0 UNDEFINED -41 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 419 6 1 5 5.6 CCOc1cc(CN2CCC(Nc3nc4ccc(Cl)cc4o3)CC2)ccc1Cl None
46882227 12948 0 UNDEFINED -57 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 540 10 2 10 3.8 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5cn(C)cn5)ccc4o3)CC2)ccc1OC None
CHEMBL1081133 12948 0 UNDEFINED -57 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 540 10 2 10 3.8 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5cn(C)cn5)ccc4o3)CC2)ccc1OC None
46882517 12987 0 UNDEFINED -32 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 398 7 1 7 4.2 CCOc1cc(CN2CCC(Nc3nc4cccnc4s3)CC2)ccc1OC None
CHEMBL1081317 12987 0 UNDEFINED -32 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 398 7 1 7 4.2 CCOc1cc(CN2CCC(Nc3nc4cccnc4s3)CC2)ccc1OC None
46882224 13120 0 UNDEFINED -181 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 543 10 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)cc(OC2CCOCC2)c1 None
CHEMBL1082036 13120 0 UNDEFINED -181 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 543 10 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)cc(OC2CCOCC2)c1 None
46882516 13121 0 UNDEFINED -27 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 431 7 1 6 5.4 CCOc1cc(CN2CCC(Nc3nc4ccc(Cl)cc4s3)CC2)ccc1OC None
CHEMBL1082040 13121 0 UNDEFINED -27 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 431 7 1 6 5.4 CCOc1cc(CN2CCC(Nc3nc4ccc(Cl)cc4s3)CC2)ccc1OC None
11848624 95921 0 UNDEFINED -245 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
CHEMBL236587 95921 0 UNDEFINED -245 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
24740752 95922 0 UNDEFINED -436 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 409 8 1 6 4.9 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCC(C)C None
CHEMBL236588 95922 0 UNDEFINED -436 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 409 8 1 6 4.9 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCC(C)C None
24740863 95933 0 UNDEFINED -134 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl None
CHEMBL236610 95933 0 UNDEFINED -134 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl None
24740864 95934 0 UNDEFINED -269 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 365 6 1 5 4.6 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1C None
CHEMBL236611 95934 0 UNDEFINED -269 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 365 6 1 5 4.6 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1C None
11848679 96019 0 UNDEFINED -776 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 489 9 3 9 2.9 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)cc(OCC)c1N None
CHEMBL236788 96019 0 UNDEFINED -776 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 489 9 3 9 2.9 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)cc(OCC)c1N None
24740750 96482 0 UNDEFINED -151 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 6 4.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1O None
CHEMBL237660 96482 0 UNDEFINED -151 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 6 4.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1O None
24740753 152895 0 UNDEFINED -33 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 8 1 6 4.7 CCCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
CHEMBL391951 152895 0 UNDEFINED -33 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 8 1 6 4.7 CCCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
24740751 154659 0 UNDEFINED -120 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 421 7 1 6 5.2 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OC1CCCC1 None
CHEMBL393333 154659 0 UNDEFINED -120 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 421 7 1 6 5.2 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OC1CCCC1 None
24740862 154787 0 UNDEFINED -51 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 6 1 5 4.4 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1F None
CHEMBL393436 154787 0 UNDEFINED -51 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 6 1 5 4.4 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1F None
11848677 155131 0 UNDEFINED -32 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 460 8 2 8 3.0 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)ccc1OC None
CHEMBL393718 155131 0 UNDEFINED -32 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 460 8 2 8 3.0 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)ccc1OC None
None 223127 0 125I-LTT-SST-28 -245 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 584 17 5 8 2.8 CCCCC(C(=O)NC(CCCCN)C(=O)OC)NC(=O)NC(CC1=CC=CC=C1)C(=O)NC2=CC=C(C=C2)[N+](=O)[O-] None
None 223274 0 125I-LTT-SST-28 -19952 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase None None None None None
None 224403 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 6 1 6 4.8 CCOC1=C(C=CC(=C1)NC2CCN(CC2)C3=NC4=CC=CC=C4S3)OC None
None 224404 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 397 7 1 6 4.8 CCOC1=C(C=CC(=C1)NC2CCN(CC2)CC3=NC4=CC=CC=C4S3)OC None
None 224405 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 425 7 1 6 4.6 CCOC1=C(C=CC(=C1)CN2CCC(CC2)C(=O)NC3=NC4=CC=CC=C4S3)OC None
None 224406 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 397 7 2 6 5.5 CCOC1=C(C=CC(=C1)NC2CCC(CC2)NC3=NC4=CC=CC=C4S3)OC None
None 224407 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 411 8 2 6 5.2 CCOC1=C(C=CC(=C1)NC2CCC(CC2)NCC3=NC4=CC=CC=C4S3)OC None
None 224408 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 5 1 6 4.1 CCOC1=C(C=CC(=C1)N2CCN(CC2)C(=O)NC3=NC4=CC=CC=C4S3)OC None
None 224409 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 405 8 2 6 6.1 CCOC1=C(C=CC(=C1)NCC2=CC(=CC=C2)NC3=NC4=CC=CC=C4S3)OC None
None 224410 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 382 7 1 7 3.7 CCOC1=C(C=CC(=C1)CN2CCC(CC2)NC3=NC4=C(O3)C=CC=N4)OC None
None 224411 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 380 7 2 5 4.0 CCOC1=C(C=CC(=C1)CN2CCC(CC2)NC3=NC4=CC=CC=C4N3)OC None
None 224412 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 382 7 1 7 3.7 CCOC1=C(N=CC(=C1)CN2CCC(CC2)NC3=NC4=CC=CC=C4O3)OC None
None 224413 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 409 8 1 6 5.1 CCOC1=C(C=CC(=C1)CN2CCC(CC2)NC3=NC4=CC=CC=C4O3)OC(C)C None
None 224414 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 413 8 1 6 4.8 CCOC1=CC(=C(C(=C1)CN2CCC(CC2)NC3=NC4=CC=CC=C4O3)F)OCC None
None 224415 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 429 9 2 7 3.8 CCOC1=C(C=C(C(=C1)CN2CCC(CC2)NC3=NC4=CC=CC=C4O3)F)OCCO None
2054 10746 15 125I-CGP23996 -446 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 125I-CGP23996 -446 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 125I-CGP23996 -446 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 125I-CGP23996 -446 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 125I-CGP23996 -446 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
None 222876 0 125I-LTT-SST-28 -1288 12 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
13105142 222877 0 UNDEFINED -23442 5 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 808 11 8 8 2.0 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O None
2054 10746 15 125I-SRIF-28 -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 125I-SRIF-28 -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 125I-SRIF-28 -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 125I-SRIF-28 -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 125I-SRIF-28 -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 10746 15 125I-SRIF -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 125I-SRIF -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 125I-SRIF -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 125I-SRIF -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 125I-SRIF -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
None 223125 0 125I-Tyr11-somatostatin-14 -57 9 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 1077 14 12 13 0.6 CC(C1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=CC=C4)CC5=CC=CC=C5)N)C(=O)N)CC6=CC=CC=C6)O None
None 223125 0 UNDEFINED -57 9 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 1077 14 12 13 0.6 CC(C1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=CC=C4)CC5=CC=CC=C5)N)C(=O)N)CC6=CC=CC=C6)O None
2054 10746 15 125I-Tyr11-SRIF -575 11 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 125I-Tyr11-SRIF -575 11 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 125I-Tyr11-SRIF -575 11 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 125I-Tyr11-SRIF -575 11 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 125I-Tyr11-SRIF -575 11 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 125I-Tyr10-CST14 -501 14 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-Tyr10-CST14 -501 14 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
448601 9682 48 125I-Tyr10-CST14 -501 14 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-Tyr10-CST14 -501 14 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-Tyr10-CST14 -501 14 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-Tyr10-CST14 -501 14 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-Tyr10-CST14 -501 14 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
None 223125 0 125I-SOMATOSTATIN -57 9 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 1077 14 12 13 0.6 CC(C1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=CC=C4)CC5=CC=CC=C5)N)C(=O)N)CC6=CC=CC=C6)O None
2055 9682 48 125I-Tyr11-SRIF -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-Tyr11-SRIF -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
448601 9682 48 125I-Tyr11-SRIF -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-Tyr11-SRIF -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-Tyr11-SRIF -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-Tyr11-SRIF -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-Tyr11-SRIF -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 222875 0 125I-Tyr11-SRIF -18 13 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-Tyr11-SRIF -9 13 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
2055 9682 48 125I-LTT-SST-28 -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-LTT-SST-28 -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
448601 9682 48 125I-LTT-SST-28 -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-LTT-SST-28 -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-LTT-SST-28 -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-LTT-SST-28 -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-LTT-SST-28 -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 10746 15 125I-Tyr10-CST14 -446 11 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 125I-Tyr10-CST14 -446 11 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 125I-Tyr10-CST14 -446 11 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 125I-Tyr10-CST14 -446 11 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 125I-Tyr10-CST14 -446 11 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
None 223126 0 125I-LTT-SST-28 -6165 5 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 585 8 5 5 4.2 CC(C1=CNC2=CC=CC=C21)C(C(=O)NCC3CCCC(C3)CN)NC(=O)N4CCC(CC4)N5C6=CC=CC=C6NC5=O None
None 223126 0 UNDEFINED -6165 5 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 585 8 5 5 4.2 CC(C1=CNC2=CC=CC=C21)C(C(=O)NCC3CCCC(C3)CN)NC(=O)N4CCC(CC4)N5C6=CC=CC=C6NC5=O None
None 222876 0 125I-Tyr11-SRIF -1288 12 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
2054 10746 15 125I-SOMATOSTATIN -446 11 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 125I-SOMATOSTATIN -446 11 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 125I-SOMATOSTATIN -446 11 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 125I-SOMATOSTATIN -446 11 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 125I-SOMATOSTATIN -446 11 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
448601 9682 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
448601 9682 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 222875 0 125I-Tyr10-CST14 -9 13 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
13105142 222877 0 125I-LTT-SRIF28 -23442 5 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 808 11 8 8 2.0 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O None
13105142 222877 0 125I-LTT-SRIF28 -23442 5 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 808 11 8 8 2.0 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O None
2054 10746 15 125I-LTT-SST-28 -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 10746 15 UNDEFINED -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 125I-LTT-SST-28 -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 UNDEFINED -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 125I-LTT-SST-28 -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 UNDEFINED -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 125I-LTT-SST-28 -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 UNDEFINED -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 125I-LTT-SST-28 -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 UNDEFINED -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
None 222876 0 125I-LTT-SST-28 -1288 12 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 222876 0 125I-CGP23996 -38 12 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
2054 10746 15 125I-LTT-SRIF28 -446 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 125I-LTT-SRIF28 -446 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 125I-LTT-SRIF28 -446 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 125I-LTT-SRIF28 -446 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 125I-LTT-SRIF28 -446 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 None -501 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
383414 9682 48 None -501 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
448601 9682 48 None -501 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
90488715 9682 48 None -501 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
CHEMBL1680 9682 48 None -501 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
CHEMBL262746 9682 48 None -501 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
DB00104 9682 48 None -501 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
None 222876 0 125I-LTT-SST-28 -1288 12 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
16161315 222875 0 125I-Tyr11-SRIF -18 13 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
2031 9053 0 UNDEFINED -112 9 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase None None None None None
71349 9053 0 UNDEFINED -112 9 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB06791 9053 0 UNDEFINED -112 9 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase None None None None None
None 222876 0 125I-Tyr11-SRIF -1288 12 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 222876 0 125I-Tyr11-SRIF -38 12 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
2055 9682 48 125I-Tyr11-somatostatin-14 -501 14 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-Tyr11-somatostatin-14 -501 14 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase None None None None None
448601 9682 48 125I-Tyr11-somatostatin-14 -501 14 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-Tyr11-somatostatin-14 -501 14 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-Tyr11-somatostatin-14 -501 14 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-Tyr11-somatostatin-14 -501 14 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-Tyr11-somatostatin-14 -501 14 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase None None None None None
13105142 222877 0 125I-Tyr10-CST14 -23442 5 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 808 11 8 8 2.0 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O None
None 223129 0 125I-LTT-SST-28 -112 5 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 536 11 4 5 5.2 CC(COC(=O)C(CCCCN)NC(=O)CC1=C(NC2=C1C=CC3=CC=CC=C32)C4=CC5=CC=CC=C5C=C4)N None
None 223129 0 UNDEFINED -112 5 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 536 11 4 5 5.2 CC(COC(=O)C(CCCCN)NC(=O)CC1=C(NC2=C1C=CC3=CC=CC=C32)C4=CC5=CC=CC=C5C=C4)N None
None 223127 0 125I-LTT-SST-28 -245 5 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 584 17 5 8 2.8 CCCCC(C(=O)NC(CCCCN)C(=O)OC)NC(=O)NC(CC1=CC=CC=C1)C(=O)NC2=CC=C(C=C2)[N+](=O)[O-] None
None 223127 0 UNDEFINED -245 5 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 584 17 5 8 2.8 CCCCC(C(=O)NC(CCCCN)C(=O)OC)NC(=O)NC(CC1=CC=CC=C1)C(=O)NC2=CC=C(C=C2)[N+](=O)[O-] None
16161315 222875 0 None -9 13 Human 8.0 pKi = 8.0 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 receptor expressed in CHO cells
Drug Central 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
13105142 222877 0 125I-CGP23996 -23442 5 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 808 11 8 8 2.0 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O None
2055 9682 48 125I-CGP23996 -501 14 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-CGP23996 -501 14 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase None None None None None
448601 9682 48 125I-CGP23996 -501 14 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-CGP23996 -501 14 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-CGP23996 -501 14 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-CGP23996 -501 14 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-CGP23996 -501 14 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase None None None None None
2028 8288 0 None -398 6 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12616335
2014 8995 0 None -35 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2014 8995 0 None -35 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2040 7435 0 None -6 4 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
3513 9620 0 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 11 3 4 5.2 O=C(NCCCc1cnc[nH]1)NCCCN(c1ccc(cn1)Br)Cc1ccc(c(c1)Cl)Cl 9822540
5311371 9620 0 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 11 3 4 5.2 O=C(NCCCc1cnc[nH]1)NCCCN(c1ccc(cn1)Br)Cc1ccc(c(c1)Cl)Cl 9822540
CHEMBL1474351 9620 0 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 11 3 4 5.2 O=C(NCCCc1cnc[nH]1)NCCCN(c1ccc(cn1)Br)Cc1ccc(c(c1)Cl)Cl 9822540
2004 7429 0 None -4 7 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2069 7439 0 None 1 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
16130961 7678 0 None -2 6 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
16130961 7678 0 None -2 6 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2005 7678 0 None -2 6 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2005 7678 0 None -2 6 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2007 7953 0 None -6 6 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2007 7953 0 None -6 6 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
10115 8891 14 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 468 10 4 5 1.4 NCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NS(=O)(=O)c1ccc(c2c1cccc2)C 15333679
11442741 8891 14 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 468 10 4 5 1.4 NCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NS(=O)(=O)c1ccc(c2c1cccc2)C 15333679
CHEMBL4451852 8891 14 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 468 10 4 5 1.4 NCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NS(=O)(=O)c1ccc(c2c1cccc2)C 15333679
2082 9039 14 None 7079 2 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 9784130
5311374 9039 14 None 7079 2 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 9784130
CHEMBL1450103 9039 14 None 7079 2 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 9784130
154734381 224493 0 None -1 9 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 1095 17 13 14 0.8 CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC2=CNC3=C2C=CC=C3)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(N)=O)NC(=O)[C@@H](N)CC1=CC=C2C=CC=CC2=C1 None
2066 9940 0 None -79 4 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10354394
2029 9154 0 None -79 6 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12616335
16133849 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
16133849 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
16133849 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
16133849 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
16133849 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
16133849 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2020 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2020 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
2020 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2020 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2020 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2020 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
91935900 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
91935900 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
91935900 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
91935900 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
91935900 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
91935900 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL501796 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL501796 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
CHEMBL501796 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL501796 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL501796 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL501796 10448 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2019 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2019 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11520208
2019 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
2019 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2019 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2019 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2019 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2019 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
2019 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
44386062 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
44386062 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11520208
44386062 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
44386062 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
44386062 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
44386062 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
44386062 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
44386062 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
44386062 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
CHEMBL440072 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL440072 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11520208
CHEMBL440072 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
CHEMBL440072 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL440072 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL440072 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL440072 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL440072 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
CHEMBL440072 10447 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
2008 7994 0 None -1 6 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2008 7994 0 None -1 6 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799