Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
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
72943279 184835 0 None - 1 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 425 3 2 4 5.5 Cc1cc(C)cc(-c2cncc(-c3nc4cc(C)cc(C)c4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
CHEMBL4861425 184835 0 None - 1 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 425 3 2 4 5.5 Cc1cc(C)cc(-c2cncc(-c3nc4cc(C)cc(C)c4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
164624123 185163 0 None - 1 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 415 3 2 4 5.0 Cc1cc(C)cc(-c2cncc(-c3nc4cc(F)ccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
CHEMBL4866325 185163 0 None - 1 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 415 3 2 4 5.0 Cc1cc(C)cc(-c2cncc(-c3nc4cc(F)ccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
164623072 185583 0 None - 1 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 411 3 2 4 5.1 Cc1cc(C)cc(-c2cncc(-c3nc4cc(C)ccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
CHEMBL4872591 185583 0 None - 1 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 411 3 2 4 5.1 Cc1cc(C)cc(-c2cncc(-c3nc4cc(C)ccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
164610567 184080 0 None - 1 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 465 3 2 4 5.9 Cc1cc(C)cc(-c2cncc(-c3nc4cc(C(F)(F)F)ccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
CHEMBL4849848 184080 0 None - 1 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 465 3 2 4 5.9 Cc1cc(C)cc(-c2cncc(-c3nc4cc(C(F)(F)F)ccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
164614320 184794 0 None - 1 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 431 3 2 4 5.5 Cc1cc(C)cc(-c2cncc(-c3nc4cc(Cl)ccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
CHEMBL4860633 184794 0 None - 1 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 431 3 2 4 5.5 Cc1cc(C)cc(-c2cncc(-c3nc4cc(Cl)ccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
118057812 185628 0 None - 1 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 431 4 2 5 4.7 COc1cc(F)cc(-c2cncc(-c3nc4cc(C)ccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
CHEMBL4873269 185628 0 None - 1 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 431 4 2 5 4.7 COc1cc(F)cc(-c2cncc(-c3nc4cc(C)ccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
118057816 184319 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 419 3 2 4 4.8 Cc1cc(F)cc(-c2cncc(-c3nc4cc(F)ccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
CHEMBL4853282 184319 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 419 3 2 4 4.8 Cc1cc(F)cc(-c2cncc(-c3nc4cc(F)ccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
164615920 184683 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 422 3 2 5 4.7 Cc1cc(C)cc(-c2cncc(-c3nc4cc(C#N)ccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
CHEMBL4858892 184683 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 422 3 2 5 4.7 Cc1cc(C)cc(-c2cncc(-c3nc4cc(C#N)ccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
2055 2851 43 None 8 5 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL None None None None 10.1016/j.bmc.2021.116424
383414 2851 43 None 8 5 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL None None None None 10.1016/j.bmc.2021.116424
90488715 2851 43 None 8 5 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL None None None None 10.1016/j.bmc.2021.116424
CHEMBL1680 2851 43 None 8 5 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL None None None None 10.1016/j.bmc.2021.116424
CHEMBL262746 2851 43 None 8 5 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL None None None None 10.1016/j.bmc.2021.116424
DB00104 2851 43 None 8 5 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL None None None None 10.1016/j.bmc.2021.116424
72943278 185012 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 428 4 2 4 5.2 Cc1cc(C)cc(NC(=O)c2cncc(-c3cc(C)cc(C)c3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
CHEMBL4863880 185012 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 428 4 2 4 5.2 Cc1cc(C)cc(NC(=O)c2cncc(-c3cc(C)cc(C)c3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
118057665 183809 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 428 4 2 4 5.2 Cc1cc(C)cc(C(=O)Nc2cncc(-c3cc(C)cc(C)c3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
CHEMBL4845867 183809 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 428 4 2 4 5.2 Cc1cc(C)cc(C(=O)Nc2cncc(-c3cc(C)cc(C)c3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
164624692 185454 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 458 4 2 6 4.3 Cc1cc(C(=O)Nc2cncc(-c3cc(Cl)cc(Cl)c3)c2N2CCC(N)CC2)n(C)n1 10.1016/j.bmc.2021.116424
CHEMBL4870834 185454 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 458 4 2 6 4.3 Cc1cc(C(=O)Nc2cncc(-c3cc(Cl)cc(Cl)c3)c2N2CCC(N)CC2)n(C)n1 10.1016/j.bmc.2021.116424
164622117 184892 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 443 5 2 6 4.5 COc1cc(OC)cc(-c2cncc(-c3nc4cc(C)ccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
CHEMBL4862195 184892 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 443 5 2 6 4.5 COc1cc(OC)cc(-c2cncc(-c3nc4cc(C)ccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
118057675 185836 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 435 4 2 5 4.5 COc1cc(F)cc(-c2cncc(-c3nc4cc(F)ccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
CHEMBL4876263 185836 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 435 4 2 5 4.5 COc1cc(F)cc(-c2cncc(-c3nc4cc(F)ccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
118057538 184233 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 397 3 2 4 4.8 Cc1cc(C)cc(-c2cncc(-c3nc4ccccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
CHEMBL4851978 184233 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 397 3 2 4 4.8 Cc1cc(C)cc(-c2cncc(-c3nc4ccccc4[nH]3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
164627529 186015 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 439 3 2 4 5.2 NC1CCN(c2c(-c3cc(F)cc(Cl)c3)cncc2-c2nc3cc(F)ccc3[nH]2)CC1 10.1016/j.bmc.2021.116424
CHEMBL4878917 186015 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 439 3 2 4 5.2 NC1CCN(c2c(-c3cc(F)cc(Cl)c3)cncc2-c2nc3cc(F)ccc3[nH]2)CC1 10.1016/j.bmc.2021.116424
164614581 184408 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 512 4 2 6 5.0 Cn1ncc(C(=O)Nc2cncc(-c3cc(Cl)cc(Cl)c3)c2N2CCC(N)CC2)c1C(F)(F)F 10.1016/j.bmc.2021.116424
CHEMBL4854548 184408 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 512 4 2 6 5.0 Cn1ncc(C(=O)Nc2cncc(-c3cc(Cl)cc(Cl)c3)c2N2CCC(N)CC2)c1C(F)(F)F 10.1016/j.bmc.2021.116424
16129706 207277 36 None -4 10 Human 10.0 pEC50 = 10 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 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 10.1016/j.bmcl.2005.05.061
CHEMBL1823872 207277 36 None -4 10 Human 10.0 pEC50 = 10 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 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 10.1016/j.bmcl.2005.05.061
162666722 181654 0 None -2 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(F)c4O)cc3C2C(=O)N(C)CC2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4783565 181654 0 None -2 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(F)c4O)cc3C2C(=O)N(C)CC2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762567 179687 0 None 64 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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 179687 0 None 64 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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
164624443 184913 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 458 4 2 6 4.3 Cc1nn(C)cc1C(=O)Nc1cncc(-c2cc(Cl)cc(Cl)c2)c1N1CCC(N)CC1 10.1016/j.bmc.2021.116424
CHEMBL4862497 184913 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 458 4 2 6 4.3 Cc1nn(C)cc1C(=O)Nc1cncc(-c2cc(Cl)cc(Cl)c2)c1N1CCC(N)CC1 10.1016/j.bmc.2021.116424
140762567 179687 0 None 64 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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 179687 0 None 64 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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
164625441 184928 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 480 4 2 6 4.9 NC1CCN(c2c(NC(=O)c3cn4ccccc4n3)cncc2-c2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmc.2021.116424
CHEMBL4862717 184928 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 480 4 2 6 4.9 NC1CCN(c2c(NC(=O)c3cn4ccccc4n3)cncc2-c2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmc.2021.116424
140762568 180672 0 None 51 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 547 6 2 5 5.3 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)cc(C(N)=O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4761949 180672 0 None 51 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 547 6 2 5 5.3 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)cc(C(N)=O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762568 180672 0 None 51 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 547 6 2 5 5.3 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)cc(C(N)=O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4761949 180672 0 None 51 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 547 6 2 5 5.3 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)cc(C(N)=O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762573 181785 0 None 79 4 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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 181785 0 None 79 4 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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
164610738 184387 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 440 4 2 4 5.2 NC1CCN(c2c(NC(=O)c3ccccc3)cncc2-c2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmc.2021.116424
CHEMBL4854239 184387 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 440 4 2 4 5.2 NC1CCN(c2c(NC(=O)c3ccccc3)cncc2-c2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmc.2021.116424
139392666 189598 0 None -1 5 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat SST5Agonist activity at rat SST5
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 189598 0 None -1 5 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat SST5Agonist activity at rat SST5
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
124174645 181942 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 502 5 2 5 5.8 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4787292 181942 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 502 5 2 5 5.8 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
139392666 189598 0 None -1 5 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat SST5Agonist activity at rat SST5
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 189598 0 None -1 5 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat SST5Agonist activity at rat SST5
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
124174645 181942 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 502 5 2 5 5.8 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4787292 181942 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 502 5 2 5 5.8 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762551 179778 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 527 5 2 6 5.6 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(O)cc(C#N)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4751583 179778 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 527 5 2 6 5.6 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(O)cc(C#N)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
139392804 190997 1 None 1 5 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat SST5Agonist activity at rat SST5
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 190997 1 None 1 5 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat SST5Agonist activity at rat SST5
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
140762551 179778 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 527 5 2 6 5.6 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(O)cc(C#N)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4751583 179778 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 527 5 2 6 5.6 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(O)cc(C#N)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
162645609 178940 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 537 6 2 7 5.0 Cc1cc(C)cc(-c2cnc3ncn(-c4cc(O)cc(C(F)(F)F)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4741372 178940 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 537 6 2 7 5.0 Cc1cc(C)cc(-c2cnc3ncn(-c4cc(O)cc(C(F)(F)F)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
139392804 190997 1 None 1 5 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat SST5Agonist activity at rat SST5
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 190997 1 None 1 5 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat SST5Agonist activity at rat SST5
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
162645609 178940 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 537 6 2 7 5.0 Cc1cc(C)cc(-c2cnc3ncn(-c4cc(O)cc(C(F)(F)F)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4741372 178940 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 537 6 2 7 5.0 Cc1cc(C)cc(-c2cnc3ncn(-c4cc(O)cc(C(F)(F)F)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
164613012 184524 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 459 4 2 6 4.8 Cc1nc(C(=O)Nc2cncc(-c3cc(Cl)cc(Cl)c3)c2N2CCC(N)CC2)c(C)o1 10.1016/j.bmc.2021.116424
CHEMBL4856293 184524 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 459 4 2 6 4.8 Cc1nc(C(=O)Nc2cncc(-c3cc(Cl)cc(Cl)c3)c2N2CCC(N)CC2)c(C)o1 10.1016/j.bmc.2021.116424
124168080 181242 0 None -11 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
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 181242 0 None -11 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
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
118057678 184510 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 400 4 2 4 4.5 Cc1cc(C)cc(-c2cncc(NC(=O)c3ccccc3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
CHEMBL4856084 184510 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 400 4 2 4 4.5 Cc1cc(C)cc(-c2cncc(NC(=O)c3ccccc3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
162648021 179383 0 None 208 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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 179383 0 None 208 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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
162648021 179383 0 None 208 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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 179383 0 None 208 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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
90070268 185976 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 414 5 2 4 5.5 Cc1cc(C)cc(CNc2cncc(-c3cc(C)cc(C)c3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
CHEMBL4878248 185976 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 414 5 2 4 5.5 Cc1cc(C)cc(CNc2cncc(-c3cc(C)cc(C)c3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
140762563 179511 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 486 5 2 5 5.2 Cc1cc(F)cc(N2C=Nc3cc(C)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4748319 179511 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 486 5 2 5 5.2 Cc1cc(F)cc(N2C=Nc3cc(C)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762563 179511 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 486 5 2 5 5.2 Cc1cc(F)cc(N2C=Nc3cc(C)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4748319 179511 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 486 5 2 5 5.2 Cc1cc(F)cc(N2C=Nc3cc(C)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
164619752 185313 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 385 3 1 3 5.6 Cc1cc(C)cc(-c2cncc(-c3cc(C)cc(C)c3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
CHEMBL4868777 185313 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 385 3 1 3 5.6 Cc1cc(C)cc(-c2cncc(-c3cc(C)cc(C)c3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
140762295 179652 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 487 6 2 7 4.1 Cc1cc(C)cc(-c2cnc3ncn(-c4cc(O)cc(F)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4750168 179652 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 487 6 2 7 4.1 Cc1cc(C)cc(-c2cnc3ncn(-c4cc(O)cc(F)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
124167875 180030 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 489 6 2 7 4.3 Cc1cc(Cl)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4754720 180030 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 489 6 2 7 4.3 Cc1cc(Cl)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
140762470 180878 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 482 5 2 5 5.4 Cc1cc(C)cc(N2C=Nc3cc(C)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4764543 180878 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 482 5 2 5 5.4 Cc1cc(C)cc(N2C=Nc3cc(C)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762500 181141 0 None 3 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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 181141 0 None 3 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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
140762295 179652 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 487 6 2 7 4.1 Cc1cc(C)cc(-c2cnc3ncn(-c4cc(O)cc(F)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4750168 179652 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 487 6 2 7 4.1 Cc1cc(C)cc(-c2cnc3ncn(-c4cc(O)cc(F)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
124167875 180030 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 489 6 2 7 4.3 Cc1cc(Cl)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4754720 180030 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 489 6 2 7 4.3 Cc1cc(Cl)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
140762470 180878 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 482 5 2 5 5.4 Cc1cc(C)cc(N2C=Nc3cc(C)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4764543 180878 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 482 5 2 5 5.4 Cc1cc(C)cc(N2C=Nc3cc(C)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762500 181141 0 None 3 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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 181141 0 None 3 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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
140762358 179458 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 505 7 3 8 3.5 CN(Cc1c(-c2cc(Cl)cc(CO)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12)C[C@@H]1CCCN1 10.1016/j.bmcl.2020.127496
CHEMBL4747697 179458 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 505 7 3 8 3.5 CN(Cc1c(-c2cc(Cl)cc(CO)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12)C[C@@H]1CCCN1 10.1016/j.bmcl.2020.127496
140762358 179458 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 505 7 3 8 3.5 CN(Cc1c(-c2cc(Cl)cc(CO)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12)C[C@@H]1CCCN1 10.1016/j.bmcl.2020.127496
CHEMBL4747697 179458 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 505 7 3 8 3.5 CN(Cc1c(-c2cc(Cl)cc(CO)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12)C[C@@H]1CCCN1 10.1016/j.bmcl.2020.127496
156238148 181475 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)ccc4O)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4781405 181475 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)ccc4O)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762455 182067 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 490 6 2 5 5.7 CC[C@H](N)CN(C)C(=O)C1c2cc(-c3cccc(O)c3)c(Cl)cc2N=CN1c1cc(C)cc(C)c1 10.1016/j.bmcl.2020.127391
CHEMBL4788944 182067 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 490 6 2 5 5.7 CC[C@H](N)CN(C)C(=O)C1c2cc(-c3cccc(O)c3)c(Cl)cc2N=CN1c1cc(C)cc(C)c1 10.1016/j.bmcl.2020.127391
140762343 178911 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 6 2 7 4.3 Cc1cc(C)cc(-c2cnc3ncn(-c4cc(C)cc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4741139 178911 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 6 2 7 4.3 Cc1cc(C)cc(-c2cnc3ncn(-c4cc(C)cc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
162644318 181185 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 477 6 2 7 3.6 CN(Cc1c(-c2cc(F)cc(F)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12)C[C@@H]1CCCN1 10.1016/j.bmcl.2020.127496
CHEMBL4777739 181185 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 477 6 2 7 3.6 CN(Cc1c(-c2cc(F)cc(F)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12)C[C@@H]1CCCN1 10.1016/j.bmcl.2020.127496
140762341 181766 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 6 2 7 4.3 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@H]2CCCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4784765 181766 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 6 2 7 4.3 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@H]2CCCCN2)c1 10.1016/j.bmcl.2020.127496
140762569 180380 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 512 5 1 6 5.3 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cncc(C#N)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4758568 180380 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 512 5 1 6 5.3 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cncc(C#N)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762455 182067 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 490 6 2 5 5.7 CC[C@H](N)CN(C)C(=O)C1c2cc(-c3cccc(O)c3)c(Cl)cc2N=CN1c1cc(C)cc(C)c1 10.1016/j.bmcl.2020.127391
CHEMBL4788944 182067 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 490 6 2 5 5.7 CC[C@H](N)CN(C)C(=O)C1c2cc(-c3cccc(O)c3)c(Cl)cc2N=CN1c1cc(C)cc(C)c1 10.1016/j.bmcl.2020.127391
140762343 178911 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 6 2 7 4.3 Cc1cc(C)cc(-c2cnc3ncn(-c4cc(C)cc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4741139 178911 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 6 2 7 4.3 Cc1cc(C)cc(-c2cnc3ncn(-c4cc(C)cc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
140762372 179165 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 6 2 7 4.5 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CC2(N)CCCC2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4744310 179165 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 6 2 7 4.5 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CC2(N)CCCC2)c1 10.1016/j.bmcl.2020.127496
162652429 179823 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 471 6 1 6 4.4 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(F)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4752223 179823 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 471 6 1 6 4.4 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(F)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
140762569 180380 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 512 5 1 6 5.3 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cncc(C#N)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4758568 180380 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 512 5 1 6 5.3 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cncc(C#N)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
162676783 182979 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 487 6 2 7 4.1 Cc1cc(C)c(F)c(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4800376 182979 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 487 6 2 7 4.1 Cc1cc(C)c(F)c(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
162644318 181185 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 477 6 2 7 3.6 CN(Cc1c(-c2cc(F)cc(F)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12)C[C@@H]1CCCN1 10.1016/j.bmcl.2020.127496
CHEMBL4777739 181185 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 477 6 2 7 3.6 CN(Cc1c(-c2cc(F)cc(F)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12)C[C@@H]1CCCN1 10.1016/j.bmcl.2020.127496
140762484 182684 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 579 7 2 6 5.4 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(NS(C)(=O)=O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4796704 182684 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 579 7 2 6 5.4 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(NS(C)(=O)=O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762372 179165 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 6 2 7 4.5 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CC2(N)CCCC2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4744310 179165 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 6 2 7 4.5 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CC2(N)CCCC2)c1 10.1016/j.bmcl.2020.127496
140762484 182684 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 579 7 2 6 5.4 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(NS(C)(=O)=O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4796704 182684 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 579 7 2 6 5.4 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(NS(C)(=O)=O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
162676783 182979 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 487 6 2 7 4.1 Cc1cc(C)c(F)c(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4800376 182979 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 487 6 2 7 4.1 Cc1cc(C)c(F)c(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
44397389 123513 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 receptor
ChEMBL 460 9 2 6 5.2 NCCCCn1c(SCCc2c[nH]c3cc(F)ccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL363092 123513 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 receptor
ChEMBL 460 9 2 6 5.2 NCCCCn1c(SCCc2c[nH]c3cc(F)ccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
124168074 179521 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 443 7 2 7 3.6 CCN(CCN)Cc1c(-c2cc(C)cc(C)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12 10.1016/j.bmcl.2020.127496
CHEMBL4748425 179521 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 443 7 2 7 3.6 CCN(CCN)Cc1c(-c2cc(C)cc(C)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12 10.1016/j.bmcl.2020.127496
124168074 179521 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 443 7 2 7 3.6 CCN(CCN)Cc1c(-c2cc(C)cc(C)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12 10.1016/j.bmcl.2020.127496
CHEMBL4748425 179521 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 443 7 2 7 3.6 CCN(CCN)Cc1c(-c2cc(C)cc(C)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12 10.1016/j.bmcl.2020.127496
140762488 182140 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 490 5 1 6 4.8 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cnn(C)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4789848 182140 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 490 5 1 6 4.8 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cnn(C)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
162652429 179823 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 471 6 1 6 4.4 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(F)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4752223 179823 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 471 6 1 6 4.4 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(F)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
140762439 180025 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 443 6 2 7 3.5 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C(C)CN)c1 10.1016/j.bmcl.2020.127496
CHEMBL4754672 180025 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 443 6 2 7 3.5 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C(C)CN)c1 10.1016/j.bmcl.2020.127496
162666722 181654 0 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(F)c4O)cc3C2C(=O)N(C)CC2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4783565 181654 0 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(F)c4O)cc3C2C(=O)N(C)CC2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762488 182140 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 490 5 1 6 4.8 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cnn(C)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4789848 182140 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 490 5 1 6 4.8 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cnn(C)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762439 180025 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 443 6 2 7 3.5 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C(C)CN)c1 10.1016/j.bmcl.2020.127496
CHEMBL4754672 180025 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 443 6 2 7 3.5 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C(C)CN)c1 10.1016/j.bmcl.2020.127496
140762334 181092 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 510 7 2 7 3.6 CNC(=O)c1cccc(-n2cnc3ncc(-c4cc(C)cc(C)c4)c(CN(C)C[C@@H]4CCCN4)c3c2=O)c1 10.1016/j.bmcl.2020.127496
CHEMBL4776516 181092 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 510 7 2 7 3.6 CNC(=O)c1cccc(-n2cnc3ncc(-c4cc(C)cc(C)c4)c(CN(C)C[C@@H]4CCCN4)c3c2=O)c1 10.1016/j.bmcl.2020.127496
156238148 181475 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)ccc4O)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4781405 181475 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)ccc4O)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
44397706 66840 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 receptor
ChEMBL 456 9 2 6 5.4 Cc1cccc2c(CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
CHEMBL187768 66840 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 receptor
ChEMBL 456 9 2 6 5.4 Cc1cccc2c(CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
140762334 181092 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 510 7 2 7 3.6 CNC(=O)c1cccc(-n2cnc3ncc(-c4cc(C)cc(C)c4)c(CN(C)C[C@@H]4CCCN4)c3c2=O)c1 10.1016/j.bmcl.2020.127496
CHEMBL4776516 181092 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 510 7 2 7 3.6 CNC(=O)c1cccc(-n2cnc3ncc(-c4cc(C)cc(C)c4)c(CN(C)C[C@@H]4CCCN4)c3c2=O)c1 10.1016/j.bmcl.2020.127496
140762413 182989 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 493 6 2 7 4.1 CN(Cc1c(-c2cc(F)cc(Cl)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12)C[C@@H]1CCCN1 10.1016/j.bmcl.2020.127496
CHEMBL4800534 182989 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 493 6 2 7 4.1 CN(Cc1c(-c2cc(F)cc(Cl)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12)C[C@@H]1CCCN1 10.1016/j.bmcl.2020.127496
140762383 180622 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 7 2 7 3.7 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(CO)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4761276 180622 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 7 2 7 3.7 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(CO)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
139392666 189598 0 None -1047 5 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human SST2Agonist activity at human SST2
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 189598 0 None -1047 5 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human SST2Agonist activity at human SST2
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
140762383 180622 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 7 2 7 3.7 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(CO)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4761276 180622 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 7 2 7 3.7 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(CO)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
162671015 182362 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 453 6 1 6 4.2 Cc1cc(C)cc(-c2cnc3ncn(-c4ccccc4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4792889 182362 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 453 6 1 6 4.2 Cc1cc(C)cc(-c2cnc3ncn(-c4ccccc4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
140762413 182989 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 493 6 2 7 4.1 CN(Cc1c(-c2cc(F)cc(Cl)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12)C[C@@H]1CCCN1 10.1016/j.bmcl.2020.127496
CHEMBL4800534 182989 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 493 6 2 7 4.1 CN(Cc1c(-c2cc(F)cc(Cl)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12)C[C@@H]1CCCN1 10.1016/j.bmcl.2020.127496
162671015 182362 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 453 6 1 6 4.2 Cc1cc(C)cc(-c2cnc3ncn(-c4ccccc4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4792889 182362 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 453 6 1 6 4.2 Cc1cc(C)cc(-c2cnc3ncn(-c4ccccc4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
140762327 179616 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 469 6 2 7 4.0 Cc1cc(C)cc(-c2cnc3ncn(-c4ccc(O)cc4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4749667 179616 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 469 6 2 7 4.0 Cc1cc(C)cc(-c2cnc3ncn(-c4ccc(O)cc4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
140762573 181785 0 None 79 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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 181785 0 None 79 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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
162656466 180239 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 509 6 2 7 4.6 CN(Cc1c(-c2cc(Cl)cc(Cl)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12)C[C@@H]1CCCN1 10.1016/j.bmcl.2020.127496
CHEMBL4756956 180239 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 509 6 2 7 4.6 CN(Cc1c(-c2cc(Cl)cc(Cl)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12)C[C@@H]1CCCN1 10.1016/j.bmcl.2020.127496
140762445 180527 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 6 2 7 4.3 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4760476 180527 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 6 2 7 4.3 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2020.127496
140762445 180527 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 6 2 7 4.3 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4760476 180527 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 6 2 7 4.3 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2020.127496
162656466 180239 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 509 6 2 7 4.6 CN(Cc1c(-c2cc(Cl)cc(Cl)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12)C[C@@H]1CCCN1 10.1016/j.bmcl.2020.127496
CHEMBL4756956 180239 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 509 6 2 7 4.6 CN(Cc1c(-c2cc(Cl)cc(Cl)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12)C[C@@H]1CCCN1 10.1016/j.bmcl.2020.127496
140762533 179359 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 522 5 1 4 6.3 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)cc(F)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4746492 179359 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 522 5 1 4 6.3 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)cc(F)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
90070225 183814 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 415 5 1 4 5.5 Cc1cc(C)cc(OCc2cncc(-c3cc(C)cc(C)c3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
CHEMBL4845931 183814 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP AssayAgonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
ChEMBL 415 5 1 4 5.5 Cc1cc(C)cc(OCc2cncc(-c3cc(C)cc(C)c3)c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
124168105 179295 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 6 2 7 4.3 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CC2CCCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4745767 179295 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 6 2 7 4.3 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CC2CCCCN2)c1 10.1016/j.bmcl.2020.127496
140762533 179359 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 522 5 1 4 6.3 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)cc(F)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4746492 179359 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 522 5 1 4 6.3 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)cc(F)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762458 179569 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 470 6 2 5 5.4 CC[C@H](N)CN(C)C(=O)C1c2cc(-c3cccc(O)c3)c(C)cc2N=CN1c1cc(C)cc(C)c1 10.1016/j.bmcl.2020.127391
CHEMBL4748962 179569 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 470 6 2 5 5.4 CC[C@H](N)CN(C)C(=O)C1c2cc(-c3cccc(O)c3)c(C)cc2N=CN1c1cc(C)cc(C)c1 10.1016/j.bmcl.2020.127391
124168105 179295 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 6 2 7 4.3 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CC2CCCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4745767 179295 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 6 2 7 4.3 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CC2CCCCN2)c1 10.1016/j.bmcl.2020.127496
140762406 181571 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 478 6 1 7 4.1 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(C#N)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4782501 181571 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 478 6 1 7 4.1 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(C#N)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
140762406 181571 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 478 6 1 7 4.1 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(C#N)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4782501 181571 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 478 6 1 7 4.1 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(C#N)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
140762327 179616 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 469 6 2 7 4.0 Cc1cc(C)cc(-c2cnc3ncn(-c4ccc(O)cc4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4749667 179616 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 469 6 2 7 4.0 Cc1cc(C)cc(-c2cnc3ncn(-c4ccc(O)cc4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
124167759 180495 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 429 6 2 7 3.2 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CCN)c1 10.1016/j.bmcl.2020.127496
CHEMBL4760001 180495 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 429 6 2 7 3.2 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CCN)c1 10.1016/j.bmcl.2020.127496
140762468 182091 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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 10.1016/j.bmcl.2020.127391
CHEMBL4789268 182091 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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 10.1016/j.bmcl.2020.127391
140762421 180619 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 485 6 2 8 3.2 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CC2COCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4761262 180619 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 485 6 2 8 3.2 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CC2COCCN2)c1 10.1016/j.bmcl.2020.127496
162657212 180276 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 520 5 1 4 6.7 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(Cl)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4757384 180276 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 520 5 1 4 6.7 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(Cl)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
162657212 180276 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 520 5 1 4 6.7 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(Cl)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4757384 180276 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 520 5 1 4 6.7 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(Cl)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762468 182091 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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 10.1016/j.bmcl.2020.127391
CHEMBL4789268 182091 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
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 10.1016/j.bmcl.2020.127391
162651633 179585 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 457 8 2 7 3.8 CCN(CCNC)Cc1c(-c2cc(C)cc(C)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12 10.1016/j.bmcl.2020.127496
CHEMBL4749169 179585 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 457 8 2 7 3.8 CCN(CCNC)Cc1c(-c2cc(C)cc(C)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12 10.1016/j.bmcl.2020.127496
124167759 180495 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 429 6 2 7 3.2 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CCN)c1 10.1016/j.bmcl.2020.127496
CHEMBL4760001 180495 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 429 6 2 7 3.2 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CCN)c1 10.1016/j.bmcl.2020.127496
140762344 182881 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 496 7 2 7 3.3 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(C(N)=O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4799254 182881 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 496 7 2 7 3.3 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(C(N)=O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
139392804 190997 1 None -1047 5 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human SST2Agonist activity at human SST2
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 190997 1 None -1047 5 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human SST2Agonist activity at human SST2
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
140762421 180619 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 485 6 2 8 3.2 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CC2COCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4761262 180619 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 485 6 2 8 3.2 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CC2COCCN2)c1 10.1016/j.bmcl.2020.127496
11705763 167741 0 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 receptor
ChEMBL 484 10 2 7 5.4 Cc1cccc2c(C(=O)CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
CHEMBL434159 167741 0 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 receptor
ChEMBL 484 10 2 7 5.4 Cc1cccc2c(C(=O)CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
140762458 179569 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 470 6 2 5 5.4 CC[C@H](N)CN(C)C(=O)C1c2cc(-c3cccc(O)c3)c(C)cc2N=CN1c1cc(C)cc(C)c1 10.1016/j.bmcl.2020.127391
CHEMBL4748962 179569 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 470 6 2 5 5.4 CC[C@H](N)CN(C)C(=O)C1c2cc(-c3cccc(O)c3)c(C)cc2N=CN1c1cc(C)cc(C)c1 10.1016/j.bmcl.2020.127391
140762560 179539 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 542 5 3 5 5.2 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4ccc5[nH]c(=O)[nH]c5c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4748730 179539 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 542 5 3 5 5.2 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4ccc5[nH]c(=O)[nH]c5c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
124168075 181278 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 469 6 2 7 4.0 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4778857 181278 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 469 6 2 7 4.0 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
162651633 179585 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 457 8 2 7 3.8 CCN(CCNC)Cc1c(-c2cc(C)cc(C)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12 10.1016/j.bmcl.2020.127496
CHEMBL4749169 179585 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 457 8 2 7 3.8 CCN(CCNC)Cc1c(-c2cc(C)cc(C)c2)cnc2ncn(-c3cccc(O)c3)c(=O)c12 10.1016/j.bmcl.2020.127496
140762344 182881 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 496 7 2 7 3.3 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(C(N)=O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4799254 182881 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 496 7 2 7 3.3 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(C(N)=O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
122444866 184996 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SSTR2Agonist activity at human SSTR2
ChEMBL 331 2 1 3 4.4 Cc1cc(C)cc(-c2cnc3ccccc3c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
CHEMBL4863622 184996 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SSTR2Agonist activity at human SSTR2
ChEMBL 331 2 1 3 4.4 Cc1cc(C)cc(-c2cnc3ccccc3c2N2CCC(N)CC2)c1 10.1016/j.bmc.2021.116424
140762560 179539 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 542 5 3 5 5.2 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4ccc5[nH]c(=O)[nH]c5c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4748730 179539 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 542 5 3 5 5.2 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4ccc5[nH]c(=O)[nH]c5c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762459 180625 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 511 5 1 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(C#N)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4761308 180625 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 511 5 1 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(C#N)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762459 180625 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 511 5 1 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(C#N)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4761308 180625 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 511 5 1 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(C#N)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762376 180386 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 443 6 2 7 3.5 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@H](C)N)c1 10.1016/j.bmcl.2020.127496
CHEMBL4758610 180386 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 443 6 2 7 3.5 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@H](C)N)c1 10.1016/j.bmcl.2020.127496
140762530 180223 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 486 5 1 4 6.1 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4ccccc4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4756810 180223 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 486 5 1 4 6.1 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4ccccc4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762502 180264 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 554 5 1 4 7.1 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(C(F)(F)F)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4757290 180264 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 554 5 1 4 7.1 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(C(F)(F)F)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762376 180386 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 443 6 2 7 3.5 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@H](C)N)c1 10.1016/j.bmcl.2020.127496
CHEMBL4758610 180386 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 443 6 2 7 3.5 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@H](C)N)c1 10.1016/j.bmcl.2020.127496
140762502 180264 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 554 5 1 4 7.1 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(C(F)(F)F)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4757290 180264 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 554 5 1 4 7.1 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(C(F)(F)F)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762530 180223 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 486 5 1 4 6.1 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4ccccc4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4756810 180223 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 486 5 1 4 6.1 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4ccccc4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762576 179722 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 534 6 1 5 6.2 COc1cc(F)cc(-c2cc3c(cc2C)N=CN(c2cc(C)cc(Cl)c2)C3C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4751066 179722 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 534 6 1 5 6.2 COc1cc(F)cc(-c2cc3c(cc2C)N=CN(c2cc(C)cc(Cl)c2)C3C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762391 179001 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 455 6 2 7 3.6 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4742147 179001 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 455 6 2 7 3.6 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCN2)c1 10.1016/j.bmcl.2020.127496
44397835 67164 0 None 8 2 Human 8.2 pEC50 = 8.2 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 receptor
ChEMBL 476 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3ccc(Cl)cc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL189554 67164 0 None 8 2 Human 8.2 pEC50 = 8.2 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst2 receptor
ChEMBL 476 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3ccc(Cl)cc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
140762576 179722 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 534 6 1 5 6.2 COc1cc(F)cc(-c2cc3c(cc2C)N=CN(c2cc(C)cc(Cl)c2)C3C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4751066 179722 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 534 6 1 5 6.2 COc1cc(F)cc(-c2cc3c(cc2C)N=CN(c2cc(C)cc(Cl)c2)C3C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762391 179001 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 455 6 2 7 3.6 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4742147 179001 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 455 6 2 7 3.6 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCN2)c1 10.1016/j.bmcl.2020.127496
124168075 181278 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 469 6 2 7 4.0 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4778857 181278 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 469 6 2 7 4.0 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
140762429 179866 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 7 1 7 4.3 COc1cccc(-n2cnc3ncc(-c4cc(C)cc(C)c4)c(CN(C)C[C@@H]4CCCN4)c3c2=O)c1 10.1016/j.bmcl.2020.127496
CHEMBL4752814 179866 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 7 1 7 4.3 COc1cccc(-n2cnc3ncc(-c4cc(C)cc(C)c4)c(CN(C)C[C@@H]4CCCN4)c3c2=O)c1 10.1016/j.bmcl.2020.127496
140762436 178862 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 473 6 2 7 3.8 Cc1cc(F)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4740611 178862 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 473 6 2 7 3.8 Cc1cc(F)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
140762493 182625 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 529 6 2 5 5.2 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(C(N)=O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4796039 182625 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 529 6 2 5 5.2 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(C(N)=O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762510 179139 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 547 6 2 5 5.3 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(C(N)=O)ccc4F)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4744062 179139 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 547 6 2 5 5.3 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(C(N)=O)ccc4F)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762510 179139 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 547 6 2 5 5.3 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(C(N)=O)ccc4F)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4744062 179139 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 547 6 2 5 5.3 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(C(N)=O)ccc4F)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762508 182186 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 503 5 2 6 5.2 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cncc(O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4790334 182186 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 503 5 2 6 5.2 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cncc(O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762493 182625 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 529 6 2 5 5.2 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(C(N)=O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4796039 182625 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 529 6 2 5 5.2 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(C(N)=O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762436 178862 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 473 6 2 7 3.8 Cc1cc(F)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4740611 178862 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 473 6 2 7 3.8 Cc1cc(F)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
140762429 179866 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 7 1 7 4.3 COc1cccc(-n2cnc3ncc(-c4cc(C)cc(C)c4)c(CN(C)C[C@@H]4CCCN4)c3c2=O)c1 10.1016/j.bmcl.2020.127496
CHEMBL4752814 179866 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levelsAgonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL 483 7 1 7 4.3 COc1cccc(-n2cnc3ncc(-c4cc(C)cc(C)c4)c(CN(C)C[C@@H]4CCCN4)c3c2=O)c1 10.1016/j.bmcl.2020.127496
140762508 182186 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 503 5 2 6 5.2 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cncc(O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4790334 182186 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulationAgonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation
ChEMBL 503 5 2 6 5.2 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cncc(O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
52936721 60893 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 487 6 2 4 6.4 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(=O)[nH]c4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766090 60893 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 487 6 2 4 6.4 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(=O)[nH]c4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
24952323 60899 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 486 6 2 4 7.5 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(O)cc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766096 60899 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 486 6 2 4 7.5 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(O)cc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
24956953 60905 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 459 7 2 4 5.7 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccc(C(N)=O)c4)cc3c2OCCCN)c1 10.1021/jm101501b
CHEMBL1766102 60905 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 459 7 2 4 5.7 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccc(C(N)=O)c4)cc3c2OCCCN)c1 10.1021/jm101501b
24951597 60902 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 513 7 2 4 6.8 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(C(N)=O)cc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766099 60902 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 513 7 2 4 6.8 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(C(N)=O)cc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
24951598 60900 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 486 6 2 4 7.5 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccc(O)c4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766097 60900 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 486 6 2 4 7.5 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccc(O)c4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
52936724 60896 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 505 6 1 4 7.8 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(Cl)nc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766093 60896 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 505 6 1 4 7.8 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(Cl)nc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
52936831 60908 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 468 8 3 5 5.5 OCc1cccc(-c2ccc3ncc(-c4cccc(CO)c4)c(OCC[C@H]4CCCCN4)c3c2)c1 10.1021/jm101501b
CHEMBL1766105 60908 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 468 8 3 5 5.5 OCc1cccc(-c2ccc3ncc(-c4cccc(CO)c4)c(OCC[C@H]4CCCCN4)c3c2)c1 10.1021/jm101501b
44325425 111942 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutesAntagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutes
ChEMBL 639 13 4 7 3.3 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCN(S(=O)(=O)c2ccccc2)CC1 10.1016/s0960-894x(01)00568-6
CHEMBL329824 111942 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutesAntagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutes
ChEMBL 639 13 4 7 3.3 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCN(S(=O)(=O)c2ccccc2)CC1 10.1016/s0960-894x(01)00568-6
44325451 106700 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutesAntagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutes
ChEMBL 568 12 4 5 5.1 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(01)00568-6
CHEMBL316559 106700 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutesAntagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutes
ChEMBL 568 12 4 5 5.1 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(01)00568-6
24952682 60901 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 500 7 2 4 7.2 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(CO)cc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766098 60901 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 500 7 2 4 7.2 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(CO)cc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
24951595 60904 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 474 6 1 5 6.5 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cnn(C)c4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766101 60904 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 474 6 1 5 6.5 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cnn(C)c4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1021/jm101501b
44325410 205560 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutesAntagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutes
ChEMBL 604 11 4 6 3.2 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCN(C(=O)c2ccccc2)CC1 10.1016/s0960-894x(01)00568-6
CHEMBL93304 205560 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutesAntagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutes
ChEMBL 604 11 4 6 3.2 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCN(C(=O)c2ccccc2)CC1 10.1016/s0960-894x(01)00568-6
24953027 60898 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 471 6 1 4 7.1 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccncc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766095 60898 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 471 6 1 4 7.1 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccncc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
44325452 166541 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutesAntagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutes
ChEMBL 1115 17 10 13 3.8 CC(C)(C)C1N[C@H](C(=O)NC(Cc2cccc3ccccc23)C(N)=O)CSSC[C@@H](NC(=O)C(N)Cc2cccc(F)c2)C(=O)NC(Cc2cccnc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C1=O 10.1016/s0960-894x(01)00568-6
CHEMBL429000 166541 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutesAntagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutes
ChEMBL 1115 17 10 13 3.8 CC(C)(C)C1N[C@H](C(=O)NC(Cc2cccc3ccccc23)C(N)=O)CSSC[C@@H](NC(=O)C(N)Cc2cccc(F)c2)C(=O)NC(Cc2cccnc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C1=O 10.1016/s0960-894x(01)00568-6
44325478 111886 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutesAntagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutes
ChEMBL 640 12 4 7 2.8 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCN(S(=O)(=O)c2ccccc2)CC1 10.1016/s0960-894x(01)00568-6
CHEMBL329684 111886 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutesAntagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutes
ChEMBL 640 12 4 7 2.8 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCN(S(=O)(=O)c2ccccc2)CC1 10.1016/s0960-894x(01)00568-6
52936722 60894 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 486 6 2 5 6.7 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(N)nc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766091 60894 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 486 6 2 5 6.7 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(N)nc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
24953029 60897 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 489 6 1 4 7.3 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(F)nc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766094 60897 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 489 6 1 4 7.3 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(F)nc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
52936833 60903 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 474 6 1 5 6.5 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cnn(C)c4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766100 60903 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 474 6 1 5 6.5 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cnn(C)c4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
52936725 60906 19 None - 1 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 432 6 2 4 6.3 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccc(O)c4)cc3c2OCCCN)c1 10.1021/jm101501b
CHEMBL1766103 60906 19 None - 1 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 432 6 2 4 6.3 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccc(O)c4)cc3c2OCCCN)c1 10.1021/jm101501b
52936723 60895 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 501 7 1 5 7.2 COc1ccc(-c2cc3c(OCC[C@H]4CCCCN4)c(-c4cc(C)cc(C)c4)cnc3cc2Cl)cn1 10.1021/jm101501b
CHEMBL1766092 60895 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 501 7 1 5 7.2 COc1ccc(-c2cc3c(OCC[C@H]4CCCCN4)c(-c4cc(C)cc(C)c4)cnc3cc2Cl)cn1 10.1021/jm101501b
44325477 205648 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutesAntagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutes
ChEMBL 631 11 5 8 4.1 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC(n2c(O)nc3ccccc32)CC1 10.1016/s0960-894x(01)00568-6
CHEMBL93859 205648 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutesAntagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutes
ChEMBL 631 11 5 8 4.1 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC(n2c(O)nc3ccccc32)CC1 10.1016/s0960-894x(01)00568-6
44325456 112111 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutesAntagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutes
ChEMBL 507 12 4 6 0.7 COC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1cccc(F)c1)NS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(01)00568-6
CHEMBL330248 112111 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutesAntagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutes
ChEMBL 507 12 4 6 0.7 COC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1cccc(F)c1)NS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(01)00568-6
44325411 205729 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutesAntagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutes
ChEMBL 618 11 4 6 3.5 Cc1ccc(C(=O)N2CCN(C(=O)N[C@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(01)00568-6
CHEMBL94293 205729 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutesAntagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutes
ChEMBL 618 11 4 6 3.5 Cc1ccc(C(=O)N2CCN(C(=O)N[C@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(01)00568-6
54586272 60913 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 472 6 2 3 7.5 Cc1cc(C)cc(C2=C(OCCC3CCCCN3)c3cc(-c4ccccc4)c(Cl)cc3NC2)c1 10.1021/jm101501b
CHEMBL1766110 60913 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 472 6 2 3 7.5 Cc1cc(C)cc(C2=C(OCCC3CCCCN3)c3cc(-c4ccccc4)c(Cl)cc3NC2)c1 10.1021/jm101501b
44325409 205314 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutesAntagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutes
ChEMBL 654 12 4 7 3.1 Cc1ccc(S(=O)(=O)N2CCN(C(=O)N[C@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(01)00568-6
CHEMBL91696 205314 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutesAntagonistic activity towards sst2 receptor in GH4C1 cells a concentration of 1-2 x 10e6/mL incubated for 20 minutes
ChEMBL 654 12 4 7 3.1 Cc1ccc(S(=O)(=O)N2CCN(C(=O)N[C@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(01)00568-6
52936625 60892 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 471 6 1 4 7.1 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccnc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766089 60892 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 471 6 1 4 7.1 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccnc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
52936830 60907 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 476 7 2 6 5.4 Cn1cc(-c2cc3c(OCC[C@H]4CCCCN4)c(-c4cccc(CO)c4)cnc3cc2Cl)cn1 10.1021/jm101501b
CHEMBL1766104 60907 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assayAgonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
ChEMBL 476 7 2 6 5.4 Cn1cc(-c2cc3c(OCC[C@H]4CCCCN4)c(-c4cccc(CO)c4)cnc3cc2Cl)cn1 10.1021/jm101501b
2055 2851 43 None 8 5 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
383414 2851 43 None 8 5 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
90488715 2851 43 None 8 5 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
CHEMBL1680 2851 43 None 8 5 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
CHEMBL262746 2851 43 None 8 5 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
DB00104 2851 43 None 8 5 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
145705877 216005 0 None -1 5 Rat 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 1047 17 9 11 3.4 NCCCC[C@@H]1NC(=O)[C@@H](CC2=CNC3=C2C=CC=C3)NC(=O)C(NC(=O)[C@@H]2C[C@H](CN2C(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC2=CC=C(OCC3=CC=CC=C3)C=C2)NC1=O)OC(=O)NCCN)C1=CC=CC=C1 None
2050 2215 0 None - 1 Rat 10.1 pEC50 = 10.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 585 8 5 5 4.2 NC[C@@H]1CCC[C@H](C1)CNC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 15855408
5311372 2215 0 None - 1 Rat 10.1 pEC50 = 10.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 585 8 5 5 4.2 NC[C@@H]1CCC[C@H](C1)CNC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 15855408
2013 2140 0 None -91 6 Rat 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21493671
2018 2946 22 None -616 5 Rat 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21493671
9941444 2946 22 None -616 5 Rat 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21493671
CHEMBL3349607 2946 22 None -616 5 Rat 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21493671
DB06663 2946 22 None -616 5 Rat 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21493671
2018 2946 22 None -616 5 Rat 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19910453
2018 2946 22 None -616 5 Rat 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21493671
9941444 2946 22 None -616 5 Rat 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19910453
9941444 2946 22 None -616 5 Rat 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21493671
CHEMBL3349607 2946 22 None -616 5 Rat 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19910453
CHEMBL3349607 2946 22 None -616 5 Rat 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21493671
DB06663 2946 22 None -616 5 Rat 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19910453
DB06663 2946 22 None -616 5 Rat 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21493671
2019 3605 0 None -10 4 Rat 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15855408
44386062 3605 0 None -10 4 Rat 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15855408
CHEMBL440072 3605 0 None -10 4 Rat 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15855408
2013 2140 0 None -91 6 Rat 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19910453
2013 2140 0 None -91 6 Rat 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21493671
2050 2215 0 None - 1 Rat 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 585 8 5 5 4.2 NC[C@@H]1CCC[C@H](C1)CNC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 15855408
5311372 2215 0 None - 1 Rat 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 585 8 5 5 4.2 NC[C@@H]1CCC[C@H](C1)CNC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 15855408
2013 2140 0 None -91 6 Rat 5.0 pEC50 > 5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19910453
2018 2946 22 None -616 5 Rat 5.0 pEC50 > 5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19910453
9941444 2946 22 None -616 5 Rat 5.0 pEC50 > 5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19910453
CHEMBL3349607 2946 22 None -616 5 Rat 5.0 pEC50 > 5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19910453
DB06663 2946 22 None -616 5 Rat 5.0 pEC50 > 5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19910453
145705877 216005 0 None -1 5 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 1047 17 9 11 3.4 NCCCC[C@@H]1NC(=O)[C@@H](CC2=CNC3=C2C=CC=C3)NC(=O)C(NC(=O)[C@@H]2C[C@H](CN2C(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC2=CC=C(OCC3=CC=CC=C3)C=C2)NC1=O)OC(=O)NCCN)C1=CC=CC=C1 None
2017 2693 0 None 7079 2 Mouse 10.9 pIC50 = 10.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2017 2693 0 None 7079 2 Mouse 10.9 pIC50 = 10.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769370
2033 631 0 None -1 3 Human 10.9 pIC50 = 10.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8646408
2038 639 0 None - 1 Mouse 10.9 pIC50 = 10.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2033 631 0 None 1 3 Mouse 11.1 pIC50 = 11.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2033 631 0 None 1 3 Mouse 11.1 pIC50 = 11.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769370
2037 638 0 None 794 2 Mouse 11.1 pIC50 = 11.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2035 633 0 None 31622 2 Mouse 11.7 pIC50 = 11.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2049 2178 0 None - 1 Mouse 12.0 pIC50 = 12 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769370
5641 4038 0 None - 1 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18381940
2034 632 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2027 648 0 None 6 5 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11897676
2044 1494 0 None - 1 Mouse 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
5633 3534 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21082773
5640 1674 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18381940
2053 2795 0 None 3 3 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15709181
5634 3533 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21082773
5636 1332 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 16568203
5627 2798 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12009943
2039 640 0 None -3 2 Mouse 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2047 2176 0 None - 1 Mouse 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2047 2176 0 None - 1 Mouse 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769370
5638 1496 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10774879
5635 378 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20956465
5639 1672 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17225119
5647 404 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18543899
5642 2002 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12009943
5645 1434 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18543899
5643 1727 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21680701
7763 406 0 None 380 2 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18543899
2043 1306 0 None - 1 Mouse 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2013 2140 0 None -1 6 Human 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12450568
2018 2946 22 None -6 5 Human 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15477717
9941444 2946 22 None -6 5 Human 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15477717
CHEMBL3349607 2946 22 None -6 5 Human 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15477717
DB06663 2946 22 None -6 5 Human 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15477717
2042 692 0 None 5 3 Human 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15709181
5646 407 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18543899
5648 405 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18543899
16133849 3606 10 None -8 4 Mouse 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2020 3606 10 None -8 4 Mouse 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
91935900 3606 10 None -8 4 Mouse 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL501796 3606 10 None -8 4 Mouse 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2048 2177 0 None - 1 Mouse 9.4 pIC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769370
70692642 2177 0 None - 1 Mouse 9.4 pIC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769370
CHEMBL2052017 2177 0 None - 1 Mouse 9.4 pIC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769370
2052 2694 0 None - 1 Mouse 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769370
2033 631 0 None -25 3 Rat 9.7 pIC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9121614
2041 643 0 None 50 3 Human 9.7 pIC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9045884
5632 1673 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10774879
5632 1673 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17225119
2040 641 0 None 5 2 Mouse 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2026 647 0 None 1 5 Human 7.5 pIC50 None 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11897676




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
140762567 179687 0 None - 0 Human 9.9 pEC50 = 9.9 Binding
Agonist activity at SST2 (unknown origin)Agonist activity at SST2 (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 179687 0 None - 0 Human 9.9 pEC50 = 9.9 Binding
Agonist activity at SST2 (unknown origin)Agonist activity at SST2 (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
140762568 180672 0 None - 0 Human 9.8 pEC50 = 9.8 Binding
Agonist activity at SST2 (unknown origin)Agonist activity at SST2 (unknown origin)
ChEMBL 547 6 2 5 5.3 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)cc(C(N)=O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4761949 180672 0 None - 0 Human 9.8 pEC50 = 9.8 Binding
Agonist activity at SST2 (unknown origin)Agonist activity at SST2 (unknown origin)
ChEMBL 547 6 2 5 5.3 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)cc(C(N)=O)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762573 181785 0 None - 0 Human 9.7 pEC50 = 9.7 Binding
Agonist activity at SST2 (unknown origin)Agonist activity at SST2 (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 181785 0 None - 0 Human 9.7 pEC50 = 9.7 Binding
Agonist activity at SST2 (unknown origin)Agonist activity at SST2 (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
162666722 181654 0 None - 0 Rat 9.3 pEC50 = 9.3 Binding
Agonist activity at rat SST2Agonist activity at rat SST2
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(F)c4O)cc3C2C(=O)N(C)CC2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4783565 181654 0 None - 0 Rat 9.3 pEC50 = 9.3 Binding
Agonist activity at rat SST2Agonist activity at rat SST2
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(F)c4O)cc3C2C(=O)N(C)CC2CCCN2)c1 10.1016/j.bmcl.2020.127391
162648021 179383 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at SST2 (unknown origin)Agonist activity at SST2 (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 179383 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at SST2 (unknown origin)Agonist activity at SST2 (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
155544425 172800 0 None 436 5 Human 9.0 pEC50 = 9 Binding
Binding affinity to human SSTR2 expressed in CHO-K1 cells assessed as induction of SSTR2 internalization after 4 hrs by chemiluminescent assayBinding affinity to human SSTR2 expressed in CHO-K1 cells assessed as induction of SSTR2 internalization after 4 hrs by chemiluminescent assay
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 172800 0 None 436 5 Human 9.0 pEC50 = 9 Binding
Binding affinity to human SSTR2 expressed in CHO-K1 cells assessed as induction of SSTR2 internalization after 4 hrs by chemiluminescent assayBinding affinity to human SSTR2 expressed in CHO-K1 cells assessed as induction of SSTR2 internalization after 4 hrs by chemiluminescent assay
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
118753685 120094 0 None - 0 Human 9.0 pEC50 = 9 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
ChEMBL 1160 17 14 15 -0.5 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
CHEMBL3144288 120094 0 None - 0 Human 9.0 pEC50 = 9 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
ChEMBL 1160 17 14 15 -0.5 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
CHEMBL3546259 120094 0 None - 0 Human 9.0 pEC50 = 9 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
ChEMBL 1160 17 14 15 -0.5 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
90663872 106243 0 None - 0 Human 9.0 pEC50 = 9 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
ChEMBL 1646 26 24 30 -7.4 C[C@@H](O)[C@H](CO)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 10.1021/jm040794i
CHEMBL3144282 106243 0 None - 0 Human 9.0 pEC50 = 9 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
ChEMBL 1646 26 24 30 -7.4 C[C@@H](O)[C@H](CO)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 10.1021/jm040794i
CHEMBL3144284 106243 0 None - 0 Human 9.0 pEC50 = 9 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
ChEMBL 1646 26 24 30 -7.4 C[C@@H](O)[C@H](CO)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 10.1021/jm040794i
90663868 106241 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
ChEMBL 1484 23 21 25 -5.2 C[C@@H](O)[C@H](CO)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 10.1021/jm040794i
CHEMBL3144280 106241 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
ChEMBL 1484 23 21 25 -5.2 C[C@@H](O)[C@H](CO)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 10.1021/jm040794i
CHEMBL3144290 106241 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
ChEMBL 1484 23 21 25 -5.2 C[C@@H](O)[C@H](CO)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 10.1021/jm040794i
140762500 181141 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at SST2 (unknown origin)Agonist activity at SST2 (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 181141 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at SST2 (unknown origin)Agonist activity at SST2 (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
118753686 120095 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
ChEMBL 1322 20 18 20 -3.1 C[C@@H](O)[C@H](CO)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]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 10.1021/jm040794i
CHEMBL3144289 120095 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
ChEMBL 1322 20 18 20 -3.1 C[C@@H](O)[C@H](CO)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]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 10.1021/jm040794i
CHEMBL3546260 120095 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
ChEMBL 1322 20 18 20 -3.1 C[C@@H](O)[C@H](CO)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]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 10.1021/jm040794i
CHEMBL2372605 209975 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
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](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
CHEMBL3546216 209975 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
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](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
90663874 106245 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO 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 106245 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO 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 106245 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO 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
155563809 174817 0 None - 1 Human 8.0 pEC50 = 8.0 Binding
Binding affinity to human SSTR2 expressed in CHO-K1 cells assessed as induction of SSTR2 internalization after 4 hrs by chemiluminescent assayBinding affinity to human SSTR2 expressed in CHO-K1 cells assessed as induction of SSTR2 internalization after 4 hrs by chemiluminescent assay
ChEMBL 1987 33 15 32 5.1 CO[C@H]1C[C@H]2OC[C@@]2(OC(C)=O)[C@H]2[C@H](OC(=O)c3ccccc3)[C@]3(O)C[C@H](OC(=O)[C@H](OC(=O)OCCSSC[C@H](NC(=O)[C@@H]4CSSC[C@H](NC(=O)[C@H](N)Cc5ccccc5)C(=O)N[C@@H](Cc5ccc(O)cc5)C(=O)N[C@H](Cc5c[nH]c6ccccc56)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N4)C(N)=O)[C@@H](NC(=O)OC(C)(C)C)c4ccccc4)C(C)=C([C@@H](OC)C(=O)[C@]12C)C3(C)C 10.1021/acs.jmedchem.8b02036
CHEMBL4575530 174817 0 None - 1 Human 8.0 pEC50 = 8.0 Binding
Binding affinity to human SSTR2 expressed in CHO-K1 cells assessed as induction of SSTR2 internalization after 4 hrs by chemiluminescent assayBinding affinity to human SSTR2 expressed in CHO-K1 cells assessed as induction of SSTR2 internalization after 4 hrs by chemiluminescent assay
ChEMBL 1987 33 15 32 5.1 CO[C@H]1C[C@H]2OC[C@@]2(OC(C)=O)[C@H]2[C@H](OC(=O)c3ccccc3)[C@]3(O)C[C@H](OC(=O)[C@H](OC(=O)OCCSSC[C@H](NC(=O)[C@@H]4CSSC[C@H](NC(=O)[C@H](N)Cc5ccccc5)C(=O)N[C@@H](Cc5ccc(O)cc5)C(=O)N[C@H](Cc5c[nH]c6ccccc56)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N4)C(N)=O)[C@@H](NC(=O)OC(C)(C)C)c4ccccc4)C(C)=C([C@@H](OC)C(=O)[C@]12C)C3(C)C 10.1021/acs.jmedchem.8b02036
90663873 106244 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO 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 106244 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO 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 106244 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO 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
16133849 3606 10 None -3 9 Human 8.6 pEC50 = 8.6 Binding
Binding affinity to human SSTR2 expressed in CHO-K1 cells assessed as induction of SSTR2 internalization after 4 hrs by chemiluminescent assayBinding affinity to human SSTR2 expressed in CHO-K1 cells assessed as induction of SSTR2 internalization after 4 hrs by chemiluminescent assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
2020 3606 10 None -3 9 Human 8.6 pEC50 = 8.6 Binding
Binding affinity to human SSTR2 expressed in CHO-K1 cells assessed as induction of SSTR2 internalization after 4 hrs by chemiluminescent assayBinding affinity to human SSTR2 expressed in CHO-K1 cells assessed as induction of SSTR2 internalization after 4 hrs by chemiluminescent assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
91935900 3606 10 None -3 9 Human 8.6 pEC50 = 8.6 Binding
Binding affinity to human SSTR2 expressed in CHO-K1 cells assessed as induction of SSTR2 internalization after 4 hrs by chemiluminescent assayBinding affinity to human SSTR2 expressed in CHO-K1 cells assessed as induction of SSTR2 internalization after 4 hrs by chemiluminescent assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
CHEMBL501796 3606 10 None -3 9 Human 8.6 pEC50 = 8.6 Binding
Binding affinity to human SSTR2 expressed in CHO-K1 cells assessed as induction of SSTR2 internalization after 4 hrs by chemiluminescent assayBinding affinity to human SSTR2 expressed in CHO-K1 cells assessed as induction of SSTR2 internalization after 4 hrs by chemiluminescent assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
CHEMBL2372606 208521 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO 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 208521 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO 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
118753688 120097 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
ChEMBL 1410 23 18 21 -2.4 C[C@@H](O)[C@H](CO)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 10.1021/jm040794i
CHEMBL3144293 120097 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
ChEMBL 1410 23 18 21 -2.4 C[C@@H](O)[C@H](CO)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 10.1021/jm040794i
CHEMBL3546262 120097 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
ChEMBL 1410 23 18 21 -2.4 C[C@@H](O)[C@H](CO)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 10.1021/jm040794i
118753687 120096 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
ChEMBL 1410 23 18 21 -2.4 C[C@@H](O)[C@H](CO)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 10.1021/jm040794i
CHEMBL3144292 120096 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
ChEMBL 1410 23 18 21 -2.4 C[C@@H](O)[C@H](CO)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 10.1021/jm040794i
CHEMBL3546261 120096 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)Relative effective concentration against human somatostatin receptor type 2 expressed in CHO cells; (n=3)
ChEMBL 1410 23 18 21 -2.4 C[C@@H](O)[C@H](CO)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 10.1021/jm040794i
124168080 181242 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human N-terminal HA-tagged SST2 expressed in cell assessed as induction of receptor internalization by colorimetric analysisAgonist activity at human N-terminal HA-tagged SST2 expressed in cell assessed as induction of receptor internalization by colorimetric analysis
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 181242 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human N-terminal HA-tagged SST2 expressed in cell assessed as induction of receptor internalization by colorimetric analysisAgonist activity at human N-terminal HA-tagged SST2 expressed in cell assessed as induction of receptor internalization by colorimetric analysis
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
13690207 114870 0 None 29 5 Human 10.7 pIC50 = 10.7 Binding
Inhibitory concentration against human somatostatin receptor type 2 in CC531 cellsInhibitory concentration against human somatostatin receptor type 2 in CC531 cells
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/jm050376t
CHEMBL3350037 114870 0 None 29 5 Human 10.7 pIC50 = 10.7 Binding
Inhibitory concentration against human somatostatin receptor type 2 in CC531 cellsInhibitory concentration against human somatostatin receptor type 2 in CC531 cells
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/jm050376t
11563877 164157 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 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 164157 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 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
10054314 163198 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 600 10 3 5 5.4 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCN(c2ccc(F)cc2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4205606 163198 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 600 10 3 5 5.4 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCN(c2ccc(F)cc2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
9959983 163317 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 581 10 3 4 6.3 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(c2ccccc2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4206924 163317 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 581 10 3 4 6.3 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(c2ccccc2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
58723865 163733 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 628 10 3 5 5.2 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCN(c2ccc(F)cc2C)C(=O)C1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4212088 163733 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 628 10 3 5 5.2 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCN(c2ccc(F)cc2C)C(=O)C1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
58723795 163948 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 614 10 3 5 4.9 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCN(c2ccc(F)cc2)C(=O)C1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4214725 163948 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 614 10 3 5 4.9 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCN(c2ccc(F)cc2)C(=O)C1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL262135 208772 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)
ChEMBL None None None None 10.1021/jm040794i
145965915 163573 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 626 9 3 5 5.0 CC(=O)c1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCN(c2ccc(F)cc2C)C(=O)C1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4210064 163573 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 626 9 3 5 5.0 CC(=O)c1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCN(c2ccc(F)cc2C)C(=O)C1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
44325477 205648 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Inhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cellsInhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cells
ChEMBL 631 11 5 8 4.1 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC(n2c(O)nc3ccccc32)CC1 10.1016/s0960-894x(01)00568-6
CHEMBL93859 205648 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Inhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cellsInhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cells
ChEMBL 631 11 5 8 4.1 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC(n2c(O)nc3ccccc32)CC1 10.1016/s0960-894x(01)00568-6
CHEMBL415860 211448 0 None - 0 Mouse 9.6 pIC50 = 9.6 Binding
Compound was tested for the inhibition of mSSTR2bCompound was tested for the inhibition of mSSTR2b
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)N1)C(=O)O 10.1021/jm960851a
13690207 114870 0 None - 5 Mouse 9.6 pIC50 = 9.6 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2bTested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2b
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 114870 0 None - 5 Mouse 9.6 pIC50 = 9.6 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2bTested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2b
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
16129706 207277 36 None - 5 Mouse 9.6 pIC50 = 9.6 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2bTested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2b
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 207277 36 None - 5 Mouse 9.6 pIC50 = 9.6 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2bTested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2b
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
145975165 163229 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 612 9 3 5 4.7 CC(=O)c1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCN(c2ccc(F)cc2)C(=O)C1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4205969 163229 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 612 9 3 5 4.7 CC(=O)c1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCN(c2ccc(F)cc2)C(=O)C1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL2369533 207877 0 None - 0 Human 9.5 pIC50 = 9.5 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 2.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 2.
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+
CHEMBL1643385 207071 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I-Tyr3]octreotide from sst2 receptor expressed in rat AR4-2J cellsDisplacement of [125I-Tyr3]octreotide from sst2 receptor expressed in rat AR4-2J cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSS[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.bmc.2010.12.014
16129706 207277 36 None 4 5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration against human somatostatin receptor type 2 in CC531 cellsInhibitory concentration against human somatostatin receptor type 2 in CC531 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/jm050376t
CHEMBL1823872 207277 36 None 4 5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration against human somatostatin receptor type 2 in CC531 cellsInhibitory concentration against human somatostatin receptor type 2 in CC531 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/jm050376t
56671558 62910 0 None - 0 Mouse 9.3 pIC50 = 9.3 Binding
Inhibition of [125I][Leu8,D-Trp22,Trp25]somatostatin-28 binding to somatostatin receptor 2Inhibition of [125I][Leu8,D-Trp22,Trp25]somatostatin-28 binding to somatostatin receptor 2
ChEMBL None None None None 10.1021/jm0496335
CHEMBL1791314 62910 0 None - 0 Mouse 9.3 pIC50 = 9.3 Binding
Inhibition of [125I][Leu8,D-Trp22,Trp25]somatostatin-28 binding to somatostatin receptor 2Inhibition of [125I][Leu8,D-Trp22,Trp25]somatostatin-28 binding to somatostatin receptor 2
ChEMBL None None None None 10.1021/jm0496335
CHEMBL2372604 208520 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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 208520 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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
11614416 163206 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 654 9 3 5 5.4 C[C@@H](c1c[nH]c2ccccc12)[C@@H](NC(=O)N1CCN(c2ccc(F)cc2)C(=O)C1)C(=O)Nc1cc(CN(C)C)ccc1OC(F)(F)F 10.1016/j.bmc.2017.09.031
CHEMBL4205696 163206 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 654 9 3 5 5.4 C[C@@H](c1c[nH]c2ccccc12)[C@@H](NC(=O)N1CCN(c2ccc(F)cc2)C(=O)C1)C(=O)Nc1cc(CN(C)C)ccc1OC(F)(F)F 10.1016/j.bmc.2017.09.031
145964683 163455 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 615 11 3 6 6.1 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)c2cccs2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4208528 163455 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 615 11 3 6 6.1 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)c2cccs2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
145966680 163691 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 587 11 3 5 5.5 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)C2CCC2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4211422 163691 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 587 11 3 5 5.5 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)C2CCC2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL264133 208852 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration against human somatostatin receptor type 2 in CC531 cellsInhibitory concentration against human somatostatin receptor type 2 in CC531 cells
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)c(I)c2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(N)c(I)c2)CSSC[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm050376t
16129706 207277 36 None 4 5 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst2 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst2 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 207277 36 None 4 5 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst2 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst2 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
145966884 163617 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 613 10 3 6 5.9 CC(=O)c1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)c2cccs2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4210627 163617 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 613 10 3 6 5.9 CC(=O)c1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)c2cccs2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
145974146 163976 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 585 10 3 5 5.3 CC(=O)c1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)C2CCC2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4215053 163976 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 585 10 3 5 5.3 CC(=O)c1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)C2CCC2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
16129706 207277 36 None 4 5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-[LTT]-SS28 from human SST2 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST2 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 207277 36 None 4 5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-[LTT]-SS28 from human SST2 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST2 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
44560907 192708 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiography
ChEMBL 1688 30 20 25 -3.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)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](Cc2ccc(O)cc2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL524341 192708 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiography
ChEMBL 1688 30 20 25 -3.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)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](Cc2ccc(O)cc2)C(N)=O)NC1=O 10.1021/jm701618q
16129706 207277 36 None 4 5 Human 9.2 pIC50 = 9.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 2Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 2
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 207277 36 None 4 5 Human 9.2 pIC50 = 9.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 2Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 2
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
25189052 12548 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12548 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12548 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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
CHEMBL526523 213903 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc(NC(N)=O)cc2)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
CHEMBL3122129 209351 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-[LTT]-SS28 from human SST2 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST2 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
90663873 106244 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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 106244 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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 106244 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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
145973735 164081 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 589 12 3 5 5.8 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)CC(C)C)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4216387 164081 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 589 12 3 5 5.8 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)CC(C)C)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
90663874 106245 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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 106245 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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 106245 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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
145975556 163061 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 588 8 3 5 4.4 CC(=O)c1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCN(C(=O)C(C)(C)C)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4203793 163061 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 588 8 3 5 4.4 CC(=O)c1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCN(C(=O)C(C)(C)C)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
13690207 114870 0 None 29 5 Human 9.0 pIC50 = 9 Binding
Binding affinity for SSTR2 receptors of rat cortex membranes was determined by using Y-labelled SMT487 radioligandBinding affinity for SSTR2 receptors of rat cortex membranes was determined by using Y-labelled SMT487 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 10.1016/s0960-894x(98)00187-5
CHEMBL3350037 114870 0 None 29 5 Human 9.0 pIC50 = 9 Binding
Binding affinity for SSTR2 receptors of rat cortex membranes was determined by using Y-labelled SMT487 radioligandBinding affinity for SSTR2 receptors of rat cortex membranes was determined by using Y-labelled SMT487 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 10.1016/s0960-894x(98)00187-5
CHEMBL3122128 209350 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-[LTT]-SS28 from human SST2 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST2 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
CHEMBL1823873 207278 7 None - 4 Human 9.0 pIC50 = 9.0 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst2 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst2 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
145978640 163416 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 575 11 3 5 5.4 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)C(C)C)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4208009 163416 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 575 11 3 5 5.4 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)C(C)C)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
90663872 106243 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)
ChEMBL 1646 26 24 30 -7.4 C[C@@H](O)[C@H](CO)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 10.1021/jm040794i
CHEMBL3144282 106243 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)
ChEMBL 1646 26 24 30 -7.4 C[C@@H](O)[C@H](CO)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 10.1021/jm040794i
CHEMBL3144284 106243 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)
ChEMBL 1646 26 24 30 -7.4 C[C@@H](O)[C@H](CO)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 10.1021/jm040794i
CHEMBL441185 212124 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibitory concentration against human somatostatin receptor type 2 in CC531 cellsInhibitory concentration against human somatostatin receptor type 2 in CC531 cells
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(N)cc2)CSSC[C@H](C(=O)N[C@H](CC(=O)O)C(N)=O)NC1=O 10.1021/jm050376t
CHEMBL499939 212323 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
90663868 106241 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)
ChEMBL 1484 23 21 25 -5.2 C[C@@H](O)[C@H](CO)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 10.1021/jm040794i
CHEMBL3144280 106241 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)
ChEMBL 1484 23 21 25 -5.2 C[C@@H](O)[C@H](CO)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 10.1021/jm040794i
CHEMBL3144290 106241 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)
ChEMBL 1484 23 21 25 -5.2 C[C@@H](O)[C@H](CO)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 10.1021/jm040794i
44290718 155335 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity of human Somatostatin receptor type 2 (hsst2) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 2 (hsst2) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL 1115 15 11 12 2.4 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)CCSSCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
CHEMBL406051 155335 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity of human Somatostatin receptor type 2 (hsst2) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 2 (hsst2) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL 1115 15 11 12 2.4 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)CCSSCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
CHEMBL498945 212305 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc(NC(N)=O)cc2)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](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
46237803 9007 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [111In]DOTA0,Tyr3]octreotide from SSTR2 receptor in rat AR42J cellsDisplacement of [111In]DOTA0,Tyr3]octreotide from SSTR2 receptor in rat AR42J cells
ChEMBL 1842 40 19 30 -2.9 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](Cc2ccccc2)NC(=O)CCCCCn2cc(COc3cccc(C(=O)NS(=O)(=O)CCNC(=O)CN4CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC4)c3)nn2)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm100246m
CHEMBL1099304 9007 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [111In]DOTA0,Tyr3]octreotide from SSTR2 receptor in rat AR42J cellsDisplacement of [111In]DOTA0,Tyr3]octreotide from SSTR2 receptor in rat AR42J cells
ChEMBL 1842 40 19 30 -2.9 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](Cc2ccccc2)NC(=O)CCCCCn2cc(COc3cccc(C(=O)NS(=O)(=O)CCNC(=O)CN4CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC4)c3)nn2)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm100246m
CHEMBL526524 213904 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](Cc2ccc(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
CHEMBL407676 210920 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration against human somatostatin receptor type 2 in CC531 cellsInhibitory concentration against human somatostatin receptor type 2 in CC531 cells
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(N)c(I)c2)CSSC[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm050376t
CHEMBL3122130 209352 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-[LTT]-SS28 from human SST2 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST2 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
CHEMBL508585 213211 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
CHEMBL441920 212142 5 None - 0 Human 8.8 pIC50 = 8.8 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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
2051 3507 20 None 2 9 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human sst2 by in vitro receptor autoradiography assayBinding affinity to human sst2 by in vitro receptor autoradiography assay
ChEMBL None None None None 10.1021/ml200032v
5311430 3507 20 None 2 9 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human sst2 by in vitro receptor autoradiography assayBinding affinity to human sst2 by in vitro receptor autoradiography assay
ChEMBL None None None None 10.1021/ml200032v
CHEMBL311695 3507 20 None 2 9 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human sst2 by in vitro receptor autoradiography assayBinding affinity to human sst2 by in vitro receptor autoradiography assay
ChEMBL None None None None 10.1021/ml200032v
CHEMBL1824052 207282 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst2 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst2 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
CHEMBL3122127 209349 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-[LTT]-SS28 from human SST2 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST2 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
91936729 167006 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)
ChEMBL None None None None 10.1021/jm040794i
CHEMBL430066 167006 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)
ChEMBL None None None None 10.1021/jm040794i
CHEMBL2372604 208520 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=5)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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 208520 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=5)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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
CHEMBL386909 210643 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibitory concentration against human somatostatin receptor type 2 in CC531 cellsInhibitory concentration against human somatostatin receptor type 2 in CC531 cells
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(N)cc2)CSSC[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm050376t
44560906 187641 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiography
ChEMBL 1722 30 19 24 -2.5 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)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
CHEMBL499446 187641 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiography
ChEMBL 1722 30 19 24 -2.5 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)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
145978229 163021 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 586 9 3 5 4.2 CC(=O)c1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCN(C(=O)C2CCC2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4203387 163021 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 586 9 3 5 4.2 CC(=O)c1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCN(C(=O)C2CCC2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL219375 207658 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst2 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst2 receptor expressed in chinese hamster CCL39 cells by autoradiography
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)N1)C(N)=O 10.1021/jm701445q
CHEMBL219375 207658 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst2 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst2 receptor by autoradiography
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)N1)C(N)=O 10.1021/jm801314f
CHEMBL386784 210635 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 2Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 2
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
CHEMBL410110 211043 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against human somatostatin receptor type 2 in CC531 cellsInhibitory concentration against human somatostatin receptor type 2 in CC531 cells
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)c(I)c2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(N)c(I)c2)CSSC[C@H](C(=O)N[C@@H](CC(=O)O)C(N)=O)NC1=O 10.1021/jm050376t
25187398 12327 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12327 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12327 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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
CHEMBL446077 212184 0 None 9 3 Human 8.0 pIC50 = 8 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
45273131 193108 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst2 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst2 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 193108 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst2 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst2 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
CHEMBL3349611 209682 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL3349617 209687 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL3349680 209707 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
49865347 15722 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST2 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST2 receptor expressed in human CCL39 cells by autoradiography
ChEMBL 1197 20 12 13 3.4 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](Cc2cccc3ccccc23)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
CHEMBL1223232 15722 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST2 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST2 receptor expressed in human CCL39 cells by autoradiography
ChEMBL 1197 20 12 13 3.4 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](Cc2cccc3ccccc23)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
CHEMBL263306 208811 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 2 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
25187400 12570 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12570 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12570 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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
16738359 136646 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 136646 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 136646 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 136646 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST2 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST2 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 136646 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST2 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST2 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 136646 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST2 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST2 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
CHEMBL1824054 207284 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst2 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst2 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](Cc2cn(Cc3ccccc3)cn2)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
CHEMBL505496 212412 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
CHEMBL3122123 209346 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-[LTT]-SS28 from human SST2 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST2 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
CHEMBL501776 212363 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
CHEMBL504462 212398 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
CHEMBL386768 210632 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)
ChEMBL None None None None 10.1021/jm040794i
CHEMBL414316 211364 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory concentration against human somatostatin receptor type 2 in CC531 cellsInhibitory concentration against human somatostatin receptor type 2 in CC531 cells
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(N)cc2)CSSC[C@H](C(=O)N[C@@H](CC(=O)O)C(N)=O)NC1=O 10.1021/jm050376t
CHEMBL2111200 207461 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 2 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
CHEMBL3349614 209685 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL3350887 209754 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL415582 211432 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 2 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 208257 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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 114928 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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 114928 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
25187681 12348 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12348 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12348 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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
CHEMBL436678 211927 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against human somatostatin receptor type 2 in CC531 cellsInhibitory concentration against human somatostatin receptor type 2 in CC531 cells
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(N)c(I)c2)CSSC[C@H](C(=O)N[C@@H](CC(=O)O)C(N)=O)NC1=O 10.1021/jm050376t
CHEMBL2372667 208525 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity of human Somatostatin receptor type 2 (hsst2) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 2 (hsst2) 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
11457521 114947 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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 114947 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL3349676 209703 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL502511 212374 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
CHEMBL506892 212435 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
44311889 96523 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Compound was tested for the inhibition of mSSTR2bCompound was tested for the inhibition of mSSTR2b
ChEMBL 1000 17 13 13 -1.4 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSC[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(=O)O 10.1021/jm960851a
CHEMBL266469 96523 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Compound was tested for the inhibition of mSSTR2bCompound was tested for the inhibition of mSSTR2b
ChEMBL 1000 17 13 13 -1.4 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSC[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(=O)O 10.1021/jm960851a
44311889 96523 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2bTested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2b
ChEMBL 1000 17 13 13 -1.4 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSC[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(=O)O 10.1021/jm960850i
CHEMBL266469 96523 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2bTested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2b
ChEMBL 1000 17 13 13 -1.4 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSC[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(=O)O 10.1021/jm960850i
CHEMBL421493 211520 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Compound was tested for the inhibition of mSSTR2bCompound was tested for the inhibition of mSSTR2b
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)O)NC1=O 10.1021/jm960851a
CHEMBL421493 211520 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2bTested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2b
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)O)NC1=O 10.1021/jm960850i
CHEMBL406816 210866 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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 207285 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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 207285 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL2371059 208251 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL1824055 207285 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst2 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst2 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
CHEMBL2079559 207441 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL2079558 207440 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
46887015 9009 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [111In]DOTA0,Tyr3]octreotide from SSTR2 receptor in rat AR42J cellsDisplacement of [111In]DOTA0,Tyr3]octreotide from SSTR2 receptor in rat AR42J cells
ChEMBL 5850 131 63 91 -1.8 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](Cc2ccccc2)NC(=O)CCCCCn2cc(COc3cc(OCc4cn(CCCCCC(=O)N[C@H](Cc5ccccc5)C(=O)N[C@H]5CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc6c[nH]c7ccccc67)NC(=O)[C@H](Cc6ccc(O)cc6)NC5=O)nn4)cc(C(=O)NCCOc4cc(OCCNC(=O)c5cc(OCc6cn(CCCCCC(=O)N[C@H](Cc7ccccc7)C(=O)N[C@H]7CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc8c[nH]c9ccccc89)NC(=O)[C@H](Cc8ccc(O)cc8)NC7=O)nn6)cc(OCc6cn(CCCCCC(=O)N[C@H](Cc7ccccc7)C(=O)N[C@H]7CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc8c[nH]c9ccccc89)NC(=O)[C@H](Cc8ccc(O)cc8)NC7=O)nn6)c5)cc(C(=O)NS(=O)(=O)CCNC(=O)CN5CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC5)c4)c3)nn2)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm100246m
CHEMBL1099306 9009 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [111In]DOTA0,Tyr3]octreotide from SSTR2 receptor in rat AR42J cellsDisplacement of [111In]DOTA0,Tyr3]octreotide from SSTR2 receptor in rat AR42J cells
ChEMBL 5850 131 63 91 -1.8 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](Cc2ccccc2)NC(=O)CCCCCn2cc(COc3cc(OCc4cn(CCCCCC(=O)N[C@H](Cc5ccccc5)C(=O)N[C@H]5CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc6c[nH]c7ccccc67)NC(=O)[C@H](Cc6ccc(O)cc6)NC5=O)nn4)cc(C(=O)NCCOc4cc(OCCNC(=O)c5cc(OCc6cn(CCCCCC(=O)N[C@H](Cc7ccccc7)C(=O)N[C@H]7CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc8c[nH]c9ccccc89)NC(=O)[C@H](Cc8ccc(O)cc8)NC7=O)nn6)cc(OCc6cn(CCCCCC(=O)N[C@H](Cc7ccccc7)C(=O)N[C@H]7CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc8c[nH]c9ccccc89)NC(=O)[C@H](Cc8ccc(O)cc8)NC7=O)nn6)c5)cc(C(=O)NS(=O)(=O)CCNC(=O)CN5CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC5)c4)c3)nn2)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm100246m
158782 157280 18 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=6)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=6)
ChEMBL 1421 26 17 22 -3.5 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](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 10.1021/jm040794i
CHEMBL408350 157280 18 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=6)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=6)
ChEMBL 1421 26 17 22 -3.5 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](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 10.1021/jm040794i
CHEMBL500326 212330 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
CHEMBL3349508 209657 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL1824051 207281 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst2 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst2 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
CHEMBL511086 213806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
CHEMBL216992 207593 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 2Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 2
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
CHEMBL3350911 209773 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
44311848 168127 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Compound was tested for the inhibition of mSSTR2bCompound was tested for the inhibition of mSSTR2b
ChEMBL 999 17 13 13 -2.0 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSC[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/jm960851a
CHEMBL436783 168127 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Compound was tested for the inhibition of mSSTR2bCompound was tested for the inhibition of mSSTR2b
ChEMBL 999 17 13 13 -2.0 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSC[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/jm960851a
44560867 188541 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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 188541 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
10577746 205511 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration required for somatostatin 2 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 2 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 205511 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration required for somatostatin 2 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 2 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
CHEMBL415585 211435 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 2 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
CHEMBL262379 208783 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 2Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 2
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
44311848 168127 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2bTested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2b
ChEMBL 999 17 13 13 -2.0 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSC[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/jm960850i
CHEMBL436783 168127 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2bTested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2b
ChEMBL 999 17 13 13 -2.0 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSC[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/jm960850i
44560866 188280 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
CHEMBL507148 188280 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
CHEMBL263209 208808 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against human somatostatin receptor type 2 in CC531 cellsInhibitory concentration against human somatostatin receptor type 2 in CC531 cells
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(N)cc2)CSSC[C@H](C(=O)N[C@@H](C(N)=O)[C@H](C)O)NC1=O 10.1021/jm050376t
CHEMBL3349666 209694 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL3350905 209768 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL2371051 208249 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 2 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 207286 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst2 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst2 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
CHEMBL3350895 209761 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL502777 212376 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
CHEMBL503036 212379 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
CHEMBL269532 209040 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against human somatostatin receptor type 2 in CC531 cellsInhibitory concentration against human somatostatin receptor type 2 in CC531 cells
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](CC(=O)O)C(N)=O)NC1=O 10.1021/jm050376t
CHEMBL3349663 209691 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL3349613 209684 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL3350896 209762 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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 209762 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
25189325 12325 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12325 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12325 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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
CHEMBL2111200 207461 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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
CHEMBL3349612 209683 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL442494 212155 0 None 1 5 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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
145977784 163045 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 616 11 3 7 5.5 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)c2nccs2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4203652 163045 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 616 11 3 7 5.5 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)c2nccs2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
145974145 163975 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 573 10 3 5 5.2 CC(=O)c1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)C(C)C)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4215052 163975 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 573 10 3 5 5.2 CC(=O)c1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)C(C)C)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
90663869 106242 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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 106242 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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
90663875 106246 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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 106246 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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
CHEMBL2372606 208521 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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 208521 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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
25187955 12315 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12315 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12315 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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
25187685 12349 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12349 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12349 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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
145977748 162973 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 588 10 3 5 4.4 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCN(C(=O)C2CCC2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4202861 162973 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 588 10 3 5 4.4 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCN(C(=O)C2CCC2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL1907758 207314 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=5)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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
90663867 106240 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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 106240 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 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
CHEMBL219375 207658 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst2Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst2
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)N1)C(N)=O 10.1021/jm060363v
56671558 56681658 62909 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Inhibition of [125I][Leu8,D-Trp22,Trp25]somatostatin-28 binding to somatostatin receptor 2Inhibition of [125I][Leu8,D-Trp22,Trp25]somatostatin-28 binding to somatostatin receptor 2
ChEMBL None None None None 10.1021/jm0496335
CHEMBL1791313 62909 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Inhibition of [125I][Leu8,D-Trp22,Trp25]somatostatin-28 binding to somatostatin receptor 2Inhibition of [125I][Leu8,D-Trp22,Trp25]somatostatin-28 binding to somatostatin receptor 2
ChEMBL None None None None 10.1021/jm0496335
CHEMBL1907758 207314 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
145976310 163085 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 599 11 3 6 5.6 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)c2ccco2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4204193 163085 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 599 11 3 6 5.6 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)c2ccco2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
145975716 163389 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 590 9 3 5 4.6 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCN(C(=O)C(C)(C)C)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4207735 163389 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 590 9 3 5 4.6 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCN(C(=O)C(C)(C)C)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL442494 212155 0 None 1 5 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 2Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 2
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
CHEMBL442494 212155 0 None 1 5 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human sst2 by in vitro receptor autoradiography assayBinding affinity to human sst2 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
CHEMBL442494 212155 0 None 1 5 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst2 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst2 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
44560905 188229 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiography
ChEMBL 1335 21 16 17 -0.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)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
CHEMBL506326 188229 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiography
ChEMBL 1335 21 16 17 -0.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)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
46237804 9008 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [111In]DOTA0,Tyr3]octreotide from SSTR2 receptor in rat AR42J cellsDisplacement of [111In]DOTA0,Tyr3]octreotide from SSTR2 receptor in rat AR42J cells
ChEMBL 3069 67 33 49 -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)cc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2ccccc2)NC(=O)CCCCCn2cc(COc3cc(OCc4cn(CCCCCC(=O)N[C@H](Cc5ccccc5)C(=O)N[C@H]5CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc6c[nH]c7ccccc67)NC(=O)[C@H](Cc6ccc(O)cc6)NC5=O)nn4)cc(C(=O)NS(=O)(=O)CCNC(=O)CN4CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC4)c3)nn2)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm100246m
CHEMBL1099305 9008 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [111In]DOTA0,Tyr3]octreotide from SSTR2 receptor in rat AR42J cellsDisplacement of [111In]DOTA0,Tyr3]octreotide from SSTR2 receptor in rat AR42J cells
ChEMBL 3069 67 33 49 -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)cc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2ccccc2)NC(=O)CCCCCn2cc(COc3cc(OCc4cn(CCCCCC(=O)N[C@H](Cc5ccccc5)C(=O)N[C@H]5CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc6c[nH]c7ccccc67)NC(=O)[C@H](Cc6ccc(O)cc6)NC5=O)nn4)cc(C(=O)NS(=O)(=O)CCNC(=O)CN4CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC4)c3)nn2)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm100246m
46887016 9010 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [111In]DOTA0,Tyr3]octreotide from SSTR2 receptor in rat AR42J cellsDisplacement of [111In]DOTA0,Tyr3]octreotide from SSTR2 receptor in rat AR42J cells
ChEMBL 1230 25 15 19 -0.6 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](Cc2ccccc2)NC(=O)CCCCCn2cc(CO)nn2)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm100246m
CHEMBL1099307 9010 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [111In]DOTA0,Tyr3]octreotide from SSTR2 receptor in rat AR42J cellsDisplacement of [111In]DOTA0,Tyr3]octreotide from SSTR2 receptor in rat AR42J cells
ChEMBL 1230 25 15 19 -0.6 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](Cc2ccccc2)NC(=O)CCCCCn2cc(CO)nn2)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm100246m
CHEMBL2372712 208528 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity of human Somatostatin receptor type 2 (hsst2) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 2 (hsst2) 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)Cc2ccccc2)CCSSCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
91936728 161166 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=7)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=7)
ChEMBL None None None None 10.1021/jm040794i
CHEMBL413647 161166 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=7)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 2 expressed in CCL39 cells; (n=7)
ChEMBL None None None None 10.1021/jm040794i
CHEMBL442494 212155 0 None 1 5 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
CHEMBL442494 212155 0 None 1 5 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst2 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst2 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
CHEMBL526498 213901 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc([N+](=O)[O-])cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
145965091 163809 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 610 11 3 6 5.4 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)c2ccccn2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL4212910 163809 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 610 11 3 6 5.4 CCOc1ccc(CN(C)C)cc1NC(=O)[C@H](NC(=O)N1CCC(C(=O)c2ccccn2)CC1)[C@@H](C)c1c[nH]c2ccccc12 10.1016/j.bmc.2017.09.031
CHEMBL1907758 207314 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 2 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
44560863 187712 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiography
ChEMBL 1346 22 16 19 -0.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc([N+](=O)[O-])cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL500477 187712 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiography
ChEMBL 1346 22 16 19 -0.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc([N+](=O)[O-])cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL442494 212155 0 None 1 5 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
145977604 163162 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 630 8 3 5 5.1 C[C@@H](c1c[nH]c2ccccc12)[C@@H](NC(=O)N1CCN(C(=O)C(C)(C)C)CC1)C(=O)Nc1cc(CN(C)C)ccc1OC(F)(F)F 10.1016/j.bmc.2017.09.031
CHEMBL4205170 163162 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR2 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 630 8 3 5 5.1 C[C@@H](c1c[nH]c2ccccc12)[C@@H](NC(=O)N1CCN(C(=O)C(C)(C)C)CC1)C(=O)Nc1cc(CN(C)C)ccc1OC(F)(F)F 10.1016/j.bmc.2017.09.031
44325478 111886 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cellsInhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cells
ChEMBL 640 12 4 7 2.8 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCN(S(=O)(=O)c2ccccc2)CC1 10.1016/s0960-894x(01)00568-6
CHEMBL329684 111886 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cellsInhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cells
ChEMBL 640 12 4 7 2.8 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCN(S(=O)(=O)c2ccccc2)CC1 10.1016/s0960-894x(01)00568-6
CHEMBL3349507 209656 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL415359 211427 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 2 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
CHEMBL265846 208912 0 None - 0 Human 6.7 pIC50 = 6.7 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 2.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 2.
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+
25189327 12572 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12572 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12572 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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
CHEMBL414446 211373 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 2 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
25187679 12547 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12547 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12547 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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
11828523 193325 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration required against human Somatostatin receptor type 2Inhibitory concentration required against human Somatostatin receptor type 2
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 193325 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration required against human Somatostatin receptor type 2Inhibitory concentration required against human Somatostatin receptor type 2
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
11343811 114949 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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 114949 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL501282 212355 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
CHEMBL509192 213550 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
CHEMBL3349664 209692 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL2371085 208256 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 2 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
45273130 193886 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst2 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst2 receptor by autoradiography
ChEMBL 1263 19 14 15 2.2 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](c3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](NC(=O)[C@@H](N)Cc3ccc(C(N)=O)cc3)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H]([C@H](C)O)NC2=O)cc1 10.1021/jm801314f
CHEMBL554976 193886 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst2 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst2 receptor by autoradiography
ChEMBL 1263 19 14 15 2.2 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](c3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](NC(=O)[C@@H](N)Cc3ccc(C(N)=O)cc3)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H]([C@H](C)O)NC2=O)cc1 10.1021/jm801314f
25187683 12330 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12330 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12330 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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
CHEMBL3350881 209748 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL3349610 209681 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL3350880 209747 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL406373 210849 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 2 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
CHEMBL3350894 209760 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL455760 212245 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst2 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst2 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
CHEMBL3350897 209763 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
44560876 188180 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiography
ChEMBL 1324 21 17 17 -0.8 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(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL505628 188180 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiography
ChEMBL 1324 21 17 17 -0.8 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(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)C(N)=O)NC1=O 10.1021/jm701618q
44325273 205567 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration required for somatostatin 2 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 2 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 205567 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration required for somatostatin 2 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 2 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
CHEMBL436962 211942 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 2Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 2
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
44290766 157401 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity of human Somatostatin receptor type 2 (hsst2) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 2 (hsst2) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL 1101 15 11 12 2.0 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)CSSCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
CHEMBL408471 157401 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity of human Somatostatin receptor type 2 (hsst2) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 2 (hsst2) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL 1101 15 11 12 2.0 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)CSSCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
CHEMBL3350889 209756 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
25188496 12413 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12413 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12413 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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
CHEMBL3349608 209680 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
25187396 12560 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12560 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12560 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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
162646037 178924 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR2 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR2 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 178924 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR2 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR2 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
44290734 155282 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity of human Somatostatin receptor type 2 (hsst2) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 2 (hsst2) 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 155282 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity of human Somatostatin receptor type 2 (hsst2) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 2 (hsst2) 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
CHEMBL442494 212155 0 None 1 5 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst2 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst2 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 212155 0 None 1 5 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST2 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST2 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
CHEMBL2011465 207359 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human sst2 by in vitro receptor autoradiography assayBinding affinity to human sst2 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)N(C)C(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)N(C)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/ml200032v
CHEMBL2372603 208519 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 5 expressed in CHO-K1 cells; (n=2)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 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
CHEMBL436892 211934 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst2Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst2
ChEMBL None None None CONC(=O)Nc1ccc(C[C@@H]2NC(=O)[C@@H](NC(=O)[C@@H](Cc3ccccc3)NC(N)=O)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)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/jm060363v
44325425 111942 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cellsInhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cells
ChEMBL 639 13 4 7 3.3 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCN(S(=O)(=O)c2ccccc2)CC1 10.1016/s0960-894x(01)00568-6
CHEMBL329824 111942 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cellsInhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cells
ChEMBL 639 13 4 7 3.3 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCN(S(=O)(=O)c2ccccc2)CC1 10.1016/s0960-894x(01)00568-6
CHEMBL1907758 207314 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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
CHEMBL447064 212188 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
CHEMBL376703 210497 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst2Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst2
ChEMBL None None None C[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)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/jm060363v
CHEMBL447658 212192 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc(NC(N)=O)cc2)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
CHEMBL524870 213839 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
CHEMBL2111257 207462 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 2 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
CHEMBL3350357 209719 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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
CHEMBL2079563 207442 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
25187953 12565 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12565 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12565 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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
CHEMBL505128 212407 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
45102042 16835 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]iodotyrosyl from human SST2 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST2 receptor expressed in CHO cells
ChEMBL 522 13 3 7 2.9 COC[C@H]1O[C@@H](OCCc2ccccc2)[C@H](NC(=O)CCCN)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254395 16835 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]iodotyrosyl from human SST2 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST2 receptor expressed in CHO cells
ChEMBL 522 13 3 7 2.9 COC[C@H]1O[C@@H](OCCc2ccccc2)[C@H](NC(=O)CCCN)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL526550 213906 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst2 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst2 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
CHEMBL3350357 209719 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 2 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 208258 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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
CHEMBL447989 212193 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
CHEMBL3349598 209671 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL3349616 209686 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL437451 211962 0 None - 0 Human 6.5 pIC50 = 6.5 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 2.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 2.
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](Cc2ccc3ccccc3c2)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+
CHEMBL3350899 209765 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL1824049 207279 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst2 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst2 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
CHEMBL3349669 209697 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL2079626 207443 2 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL3349665 209693 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
49865345 15720 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST2 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST2 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 15720 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST2 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST2 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
CHEMBL387458 210653 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 2 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
16737812 85067 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST2 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST2 receptor
ChEMBL 508 10 3 3 4.9 NCCCCCN1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm070246f
CHEMBL227211 85067 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST2 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST2 receptor
ChEMBL 508 10 3 3 4.9 NCCCCCN1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm070246f
CHEMBL2311181 207752 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
44368019 10153 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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 10153 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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
162651887 179681 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR2 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR2 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4750625 179681 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR2 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR2 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL438247 212002 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst2Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst2
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)NC1=O 10.1021/jm060363v
CHEMBL413735 211328 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity of human Somatostatin receptor type 2 (hsst2) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 2 (hsst2) 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
CHEMBL2011466 207360 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human sst2 by in vitro receptor autoradiography assayBinding affinity to human sst2 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
CHEMBL1824050 207280 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst2 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst2 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
CHEMBL451932 212213 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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](CC2CCCCC2)C(N)=O)NC1=O 10.1021/jm701618q
44325452 166541 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cellsInhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cells
ChEMBL 1115 17 10 13 3.8 CC(C)(C)C1N[C@H](C(=O)NC(Cc2cccc3ccccc23)C(N)=O)CSSC[C@@H](NC(=O)C(N)Cc2cccc(F)c2)C(=O)NC(Cc2cccnc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C1=O 10.1016/s0960-894x(01)00568-6
CHEMBL429000 166541 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cellsInhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cells
ChEMBL 1115 17 10 13 3.8 CC(C)(C)C1N[C@H](C(=O)NC(Cc2cccc3ccccc23)C(N)=O)CSSC[C@@H](NC(=O)C(N)Cc2cccc(F)c2)C(=O)NC(Cc2cccnc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C1=O 10.1016/s0960-894x(01)00568-6
CHEMBL2011464 207358 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human sst2 by in vitro receptor autoradiography assayBinding affinity to human sst2 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)NC1=O 10.1021/ml200032v
25189054 12580 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12580 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12580 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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
CHEMBL2011463 207357 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human sst2 by in vitro receptor autoradiography assayBinding affinity to human sst2 by in vitro receptor autoradiography assay
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)N(C)C1=O 10.1021/ml200032v
44325411 205729 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cellsInhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cells
ChEMBL 618 11 4 6 3.5 Cc1ccc(C(=O)N2CCN(C(=O)N[C@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(01)00568-6
CHEMBL94293 205729 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cellsInhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cells
ChEMBL 618 11 4 6 3.5 Cc1ccc(C(=O)N2CCN(C(=O)N[C@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(01)00568-6
CHEMBL453936 212227 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
CHEMBL503596 212389 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
CHEMBL455435 212240 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst2 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst2 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
CHEMBL448431 212197 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
CHEMBL3350885 209752 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL504248 212394 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
44560873 188548 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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 188548 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
10114 2509 18 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]SS-14 from human SSTR-2 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR-2 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 2509 18 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]SS-14 from human SSTR-2 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR-2 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 2509 18 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]SS-14 from human SSTR-2 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR-2 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
CHEMBL425090 211571 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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 212216 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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
CHEMBL452157 212216 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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 212216 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst2 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst2 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 212216 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
CHEMBL504395 212395 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
CHEMBL452157 212216 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]LTT-SRIF-28 from human sst2 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst2 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 212216 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 2Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 2
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
71603917 147388 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of Somatostatin receptor type 2 (unknown origin) by radioligand binding assayInhibition of Somatostatin receptor type 2 (unknown origin) by radioligand binding assay
ChEMBL 462 4 0 9 1.2 Cc1c([C@@H]2CN3CCN(C(=O)Cc4ccc(-n5cnnn5)cn4)C[C@H]3CO2)ccc(F)c1C#N 10.1016/j.bmcl.2016.10.064
CHEMBL3933749 147388 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of Somatostatin receptor type 2 (unknown origin) by radioligand binding assayInhibition of Somatostatin receptor type 2 (unknown origin) by radioligand binding assay
ChEMBL 462 4 0 9 1.2 Cc1c([C@@H]2CN3CCN(C(=O)Cc4ccc(-n5cnnn5)cn4)C[C@H]3CO2)ccc(F)c1C#N 10.1016/j.bmcl.2016.10.064
CHEMBL525030 213845 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
CHEMBL409100 210989 0 None - 0 Human 7.4 pIC50 = 7.4 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 2.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 2.
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+
CHEMBL3350912 209774 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL408338 210949 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 2Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 2
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
CHEMBL265912 208916 0 None - 0 Human 7.4 pIC50 = 7.4 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 2.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 2.
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+
118718507 114846 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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 114846 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL2011467 207361 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human sst2 by in vitro receptor autoradiography assayBinding affinity to human sst2 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)N(C)C(=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
53321995 56454 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-Tyr3]octreotide from sst2 receptor expressed in rat AR4-2J cellsDisplacement of [125I-Tyr3]octreotide from sst2 receptor expressed in rat AR4-2J cells
ChEMBL 1699 27 22 23 -3.1 C[C@H](N)C(=O)NCC(=O)N[C@H]1Cc2ccc(cc2)N=N[C@@H](Cc2cnc[nH]2)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.bmc.2010.12.014
CHEMBL1643384 56454 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-Tyr3]octreotide from sst2 receptor expressed in rat AR4-2J cellsDisplacement of [125I-Tyr3]octreotide from sst2 receptor expressed in rat AR4-2J cells
ChEMBL 1699 27 22 23 -3.1 C[C@H](N)C(=O)NCC(=O)N[C@H]1Cc2ccc(cc2)N=N[C@@H](Cc2cnc[nH]2)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.bmc.2010.12.014
44444935 94192 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst2 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst2 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 94192 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst2 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst2 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 15716 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST2 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST2 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 15716 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST2 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST2 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
CHEMBL3349597 209670 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL2011461 207355 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human sst2 by in vitro receptor autoradiography assayBinding affinity to human sst2 by in vitro receptor autoradiography assay
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)N(C)C(=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
25188220 12370 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12370 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12370 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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
70689221 77488 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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 77488 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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
CHEMBL3350883 209750 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
49865343 15718 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST2 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST2 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 15718 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST2 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST2 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
44560872 187821 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiography
ChEMBL 1677 31 18 22 -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)CCNC(=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
CHEMBL502077 187821 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiography
ChEMBL 1677 31 18 22 -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)CCNC(=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
CHEMBL3349673 209700 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
118718854 114904 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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 114904 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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 209770 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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
CHEMBL261895 208765 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 2 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
CHEMBL3350908 209771 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL3349679 209706 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
11535351 96592 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst2 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst2 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 96592 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst2 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst2 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
CHEMBL504457 212396 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
CHEMBL410047 211040 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 2Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 2
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
CHEMBL2372713 208529 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity of human Somatostatin receptor type 2 (hsst2) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 2 (hsst2) 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
CHEMBL525397 213859 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
CHEMBL524327 213816 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
CHEMBL2011462 207356 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human sst2 by in vitro receptor autoradiography assayBinding affinity to human sst2 by in vitro receptor autoradiography assay
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)N(C)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/ml200032v
CHEMBL452074 212214 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst2 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst2 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 194054 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst2 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst2 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 194054 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst2 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst2 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 213802 0 None 1 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
CHEMBL509363 213649 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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(N)=O)NC1=O 10.1021/jm701618q
CHEMBL3122124 209347 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[LTT]-SS28 from human SST2 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST2 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
CHEMBL2079559 207441 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
11468916 114951 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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 114951 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL447177 212189 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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(=O)NCC(=O)O)NC1=O 10.1021/jm701618q
CHEMBL3349674 209701 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL367125 210401 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 2Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 2
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
118718854 114904 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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 114904 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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
CHEMBL3350898 209764 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL3350891 209758 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL412629 211255 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 2.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 2.
ChEMBL None None None CNCc1ccc(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)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm010037+
CHEMBL3350893 209759 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL3350890 209757 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL3349618 209688 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL2371060 208252 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 2 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
CHEMBL3350884 209751 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL262975 208801 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 2 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
CHEMBL510901 213804 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
44368398 10154 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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 10154 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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
CHEMBL368304 210404 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 2Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 2
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)NC1=O 10.1021/jm049519m
CHEMBL219201 207654 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst2Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst2
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
CHEMBL440636 212110 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human somatostatin receptor type 2 in CC531 cellsInhibitory concentration against human somatostatin receptor type 2 in CC531 cells
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)c(I)c2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(N)cc2)CSSC[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm050376t
CHEMBL504087 212392 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
CHEMBL502219 212370 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
44325410 205560 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cellsInhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cells
ChEMBL 604 11 4 6 3.2 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCN(C(=O)c2ccccc2)CC1 10.1016/s0960-894x(01)00568-6
CHEMBL93304 205560 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cellsInhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cells
ChEMBL 604 11 4 6 3.2 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCN(C(=O)c2ccccc2)CC1 10.1016/s0960-894x(01)00568-6
52941607 16829 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]iodotyrosyl from human SST2 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST2 receptor expressed in CHO cells
ChEMBL 522 13 3 7 2.9 COC[C@H]1O[C@H](OCCc2ccccc2)[C@H](NC(=O)CCCN)[C@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254321 16829 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]iodotyrosyl from human SST2 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST2 receptor expressed in CHO cells
ChEMBL 522 13 3 7 2.9 COC[C@H]1O[C@H](OCCc2ccccc2)[C@H](NC(=O)CCCN)[C@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL3350909 209772 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
46902023 16842 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]iodotyrosyl from human SST2 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST2 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 16842 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]iodotyrosyl from human SST2 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST2 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
CHEMBL3349668 209696 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL407649 210917 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 2 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
CHEMBL2079558 207440 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL412029 211215 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst2Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst2
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
CHEMBL3349675 209702 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL3350882 209749 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL3349506 209655 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL3350886 209753 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL3349677 209704 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL3349672 209699 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
25188218 12442 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12442 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 12442 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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
CHEMBL3349671 209698 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL3349505 209654 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL446380 212186 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
53321995 56454 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I-Tyr3]octreotide from sst2 receptor expressed in rat AR4-2J cellsDisplacement of [125I-Tyr3]octreotide from sst2 receptor expressed in rat AR4-2J cells
ChEMBL 1699 27 22 23 -3.1 C[C@H](N)C(=O)NCC(=O)N[C@H]1Cc2ccc(cc2)N=N[C@@H](Cc2cnc[nH]2)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.bmc.2010.12.014
CHEMBL1643384 56454 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I-Tyr3]octreotide from sst2 receptor expressed in rat AR4-2J cellsDisplacement of [125I-Tyr3]octreotide from sst2 receptor expressed in rat AR4-2J cells
ChEMBL 1699 27 22 23 -3.1 C[C@H](N)C(=O)NCC(=O)N[C@H]1Cc2ccc(cc2)N=N[C@@H](Cc2cnc[nH]2)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.bmc.2010.12.014
CHEMBL2372699 208526 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity of human Somatostatin receptor type 2 (hsst2) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 2 (hsst2) 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
44298251 192995 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration required against human Somatostatin receptor type 2Inhibitory concentration required against human Somatostatin receptor type 2
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 192995 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration required against human Somatostatin receptor type 2Inhibitory concentration required against human Somatostatin receptor type 2
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
CHEMBL3350888 209755 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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 209755 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 2 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
CHEMBL3349678 209705 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL3351090 209788 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
CHEMBL3349667 209695 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human somatostatin 2 (hsst) receptorBinding affinity towards cloned human somatostatin 2 (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
16737814 85068 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 85068 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 85068 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst2 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 85068 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST2 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST2 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 85068 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST2 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST2 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 85068 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST2 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST2 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
44325451 106700 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cellsInhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cells
ChEMBL 568 12 4 5 5.1 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(01)00568-6
CHEMBL316559 106700 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cellsInhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cells
ChEMBL 568 12 4 5 5.1 CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(01)00568-6
49865346 15721 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST2 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST2 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
CHEMBL1223231 15721 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST2 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST2 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
CHEMBL505854 212417 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst2 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
44325409 205314 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cellsInhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cells
ChEMBL 654 12 4 7 3.1 Cc1ccc(S(=O)(=O)N2CCN(C(=O)N[C@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(01)00568-6
CHEMBL91696 205314 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cellsInhibitory concentration towards binding of sst2 receptor using [125I]somatostatin as radioligand in Neuro2A cells
ChEMBL 654 12 4 7 3.1 Cc1ccc(S(=O)(=O)N2CCN(C(=O)N[C@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(01)00568-6
CHEMBL499760 212320 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
CHEMBL505704 212415 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
49865344 15719 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST2 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST2 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 15719 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST2 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST2 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
CHEMBL498985 212308 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst2 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst2 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
CHEMBL3122125 209348 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-[LTT]-SS28 from human SST2 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST2 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](CC(N)=O)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)O)[C@@H](C)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 10.1016/j.ejmech.2013.12.003
CHEMBL263587 208823 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 2Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 2
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
CHEMBL3350906 209769 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 2 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
11642413 16904 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]iodotyrosyl from human SST2 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST2 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 16904 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]iodotyrosyl from human SST2 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST2 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
CHEMBL408752 210973 0 None 54 4 Human 9.8 pKd = 9.8 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)
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)N1)C(N)=O 10.1021/jm000361p
13690207 114870 0 None 29 5 Human 9.2 pKd = 9.2 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 receptor
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 10.1016/j.bmc.2016.08.001
CHEMBL3350037 114870 0 None 29 5 Human 9.2 pKd = 9.2 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 receptor
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 10.1016/j.bmc.2016.08.001
23656026 93817 0 None 3 2 Rat 9.1 pKd = 9.1 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 455 3 0 4 3.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250304 93817 0 None 3 2 Rat 9.1 pKd = 9.1 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 455 3 0 4 3.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL421362 211516 0 None 14 5 Human 9.1 pKd = 9.1 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst2) expressed in CHO cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst2) 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
CHEMBL407571 210912 0 None 4 4 Human 9.0 pKd = 9.0 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)
ChEMBL None None None CN[C@H](Cc1ccccc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)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](Cc2ccccc2)NC1=O 10.1021/jm000361p
CHEMBL405421 210803 0 None 12 4 Human 9.0 pKd = 9.0 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](N(C)C(=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/jm000361p
CHEMBL5078260 213753 0 None - 1 Mouse 8.8 pKd = 8.8 Binding
Binding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysisBinding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01791
CHEMBL5095749 213753 0 None - 1 Mouse 8.8 pKd = 8.8 Binding
Binding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysisBinding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01791
CHEMBL412466 211235 0 None 4 4 Human 8.7 pKd = 8.7 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)
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)[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm000361p
CHEMBL385409 210592 0 None 1 4 Human 8.0 pKd = 8.0 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)
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)N1)C(N)=O 10.1021/jm000361p
44441898 93776 0 None -1230 2 Rat 5.0 pKd = 5 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 444 3 0 5 3.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C#N)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL249932 93776 0 None -1230 2 Rat 5.0 pKd = 5 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 444 3 0 5 3.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C#N)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441885 93979 0 None -3630 2 Rat 5.0 pKd = 5 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 477 3 0 7 3.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc5nsnc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL251120 93979 0 None -3630 2 Rat 5.0 pKd = 5 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 477 3 0 7 3.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc5nsnc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441676 93569 0 None -1258 2 Rat 5.0 pKd = 5 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 510 5 0 7 3.7 COc1ccc(SC)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL248717 93569 0 None -1258 2 Rat 5.0 pKd = 5 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 510 5 0 7 3.7 COc1ccc(SC)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
44441678 93605 0 None -12022 2 Rat 5.0 pKd = 5 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 506 4 0 9 2.3 COc1ccc(C=O)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL248908 93605 0 None -12022 2 Rat 5.0 pKd = 5 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 506 4 0 9 2.3 COc1ccc(C=O)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
44441658 94015 0 None -588 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 420 3 0 5 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL251334 94015 0 None -588 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 420 3 0 5 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441870 168554 0 None -2884 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 445 3 0 6 2.3 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C#N)cn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL440233 168554 0 None -2884 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 445 3 0 6 2.3 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C#N)cn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
23656025 93647 0 None -8511 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 450 4 1 6 2.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL249113 93647 0 None -8511 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 450 4 1 6 2.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN[C@@H]1C2 10.1016/j.bmcl.2007.04.086
44441658 94015 0 None -588 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 420 3 0 5 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL251334 94015 0 None -588 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 420 3 0 5 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
44441872 93822 0 None -18 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 568 5 0 8 2.7 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ncccc4OS(=O)(=O)C(F)(F)F)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250314 93822 0 None -18 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 568 5 0 8 2.7 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ncccc4OS(=O)(=O)C(F)(F)F)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441899 153789 0 None -8511 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccc4[N+](=O)[O-])CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL398681 153789 0 None -8511 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccc4[N+](=O)[O-])CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441875 168555 0 None -1513 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 450 3 0 6 1.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(=O)n4C)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL440235 168555 0 None -1513 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 450 3 0 6 1.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(=O)n4C)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441659 154130 0 None -7762 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 538 4 0 7 2.7 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2Cc3c(cccc3OS(=O)(=O)C(F)(F)F)C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL399658 154130 0 None -7762 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 538 4 0 7 2.7 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2Cc3c(cccc3OS(=O)(=O)C(F)(F)F)C[C@H]21 10.1016/j.bmcl.2007.04.086
9871544 14086 1 None -23 11 Rat 6.9 pKd = 6.9 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST2 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST2 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 14086 1 None -23 11 Rat 6.9 pKd = 6.9 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST2 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST2 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 14086 1 None -23 11 Rat 6.9 pKd = 6.9 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST2 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST2 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
44441874 153742 0 None -1548 2 Rat 4.9 pKd = 4.9 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 436 3 1 5 1.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(=O)[nH]4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL398655 153742 0 None -1548 2 Rat 4.9 pKd = 4.9 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 436 3 1 5 1.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(=O)[nH]4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL438471 212015 0 None -15 4 Human 6.9 pKd = 6.9 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)
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)[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/jm000361p
44447048 154437 0 None -31622 2 Rat 4.9 pKd = 4.9 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 493 3 1 5 3.3 CCn1c(N2CCN(C(=O)[C@@H]3C[C@@H]4c5cccc6[nH]c(Cl)c(c56)C[C@H]4N(C)C3)CC2)cccc1=O 10.1016/j.bmcl.2007.12.030
CHEMBL401309 154437 0 None -31622 2 Rat 4.9 pKd = 4.9 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 493 3 1 5 3.3 CCn1c(N2CCN(C(=O)[C@@H]3C[C@@H]4c5cccc6[nH]c(Cl)c(c56)C[C@H]4N(C)C3)CC2)cccc1=O 10.1016/j.bmcl.2007.12.030
9849682 94498 0 None -60255 10 Human 4.9 pKd = 4.9 Binding
Binding affinity to human recombinant sst2 receptorBinding affinity to human recombinant sst2 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 94498 0 None -60255 10 Human 4.9 pKd = 4.9 Binding
Binding affinity to human recombinant sst2 receptorBinding affinity to human recombinant sst2 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
10162564 12418 0 None -21379 8 Human 4.9 pKd = 4.9 Binding
Binding affinity to human sst2 receptorBinding affinity to human sst2 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 12418 0 None -21379 8 Human 4.9 pKd = 4.9 Binding
Binding affinity to human sst2 receptorBinding affinity to human sst2 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 12418 0 None -21379 8 Human 4.9 pKd = 4.9 Binding
Binding affinity to human sst2 receptorBinding affinity to human sst2 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
44447078 94167 0 None -69 7 Rat 4.9 pKd = 4.9 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
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 94167 0 None -69 7 Rat 4.9 pKd = 4.9 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
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
44447069 94194 0 None -21379 2 Rat 4.9 pKd = 4.9 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 484 2 1 3 4.4 CN1C[C@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252428 94194 0 None -21379 2 Rat 4.9 pKd = 4.9 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 484 2 1 3 4.4 CN1C[C@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL384164 210561 0 None 6 3 Human 7.9 pKd = 7.9 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)
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)[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/jm000361p
44441902 154324 0 None -562 2 Rat 4.9 pKd = 4.9 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 487 3 0 4 4.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(C(F)(F)F)c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL400709 154324 0 None -562 2 Rat 4.9 pKd = 4.9 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 487 3 0 4 4.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(C(F)(F)F)c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44447042 94468 0 None -13489 2 Rat 4.9 pKd = 4.9 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 542 3 1 3 4.9 CCN1C[C@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL254287 94468 0 None -13489 2 Rat 4.9 pKd = 4.9 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 542 3 1 3 4.9 CCN1C[C@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44441674 154068 0 None -3890 2 Rat 4.9 pKd = 4.9 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 498 4 0 6 3.6 COc1ccc(Cl)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL399267 154068 0 None -3890 2 Rat 4.9 pKd = 4.9 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 498 4 0 6 3.6 COc1ccc(Cl)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL411017 211101 0 None 3 4 Human 7.9 pKd = 7.9 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)
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)[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm000361p
CHEMBL265636 208903 0 None 8 4 Human 7.8 pKd = 7.8 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)
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
44441881 153744 0 None -2454 2 Rat 4.9 pKd = 4.9 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 472 3 0 7 2.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nccnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL398656 153744 0 None -2454 2 Rat 4.9 pKd = 4.9 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 472 3 0 7 2.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nccnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44564784 176357 0 None -43 2 Rat 4.8 pKd = 4.8 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 485 8 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCn1c2ccccc2c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL462157 176357 0 None -43 2 Rat 4.8 pKd = 4.8 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 485 8 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCn1c2ccccc2c2ccccc21 10.1016/j.bmcl.2009.01.072
44441908 93939 0 None -91 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 477 4 0 6 2.9 COC(=O)c1ccc(N2CCN(C(=O)[C@@H]3C[C@@H]4Cc5c(cccc5OC)C[C@H]4N(C)C3)CC2)cc1 10.1016/j.bmcl.2007.04.078
CHEMBL250900 93939 0 None -91 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 477 4 0 6 2.9 COC(=O)c1ccc(N2CCN(C(=O)[C@@H]3C[C@@H]4Cc5c(cccc5OC)C[C@H]4N(C)C3)CC2)cc1 10.1016/j.bmcl.2007.04.078
44441680 93646 0 None -11 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@@H]1C[C@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL249112 93646 0 None -11 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@@H]1C[C@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@H]1C2 10.1016/j.bmcl.2007.04.086
134150680 151365 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 receptor
ChEMBL 1086 17 13 14 0.2 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(C(F)(F)F)[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1016/j.bmc.2016.08.001
CHEMBL3966064 151365 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 receptor
ChEMBL 1086 17 13 14 0.2 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(C(F)(F)F)[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1016/j.bmc.2016.08.001
46865536 11799 0 None -19 7 Rat 6.8 pKd = 6.8 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST2 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST2 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 11799 0 None -19 7 Rat 6.8 pKd = 6.8 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST2 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST2 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 11799 0 None -19 7 Rat 6.8 pKd = 6.8 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST2 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST2 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
44441664 94082 0 None -3235 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 550 4 0 8 4.3 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(cccc3OC(=O)OC(C)(C)C)C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL251751 94082 0 None -3235 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 550 4 0 8 4.3 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(cccc3OC(=O)OC(C)(C)C)C[C@H]21 10.1016/j.bmcl.2007.04.086
44564786 176232 0 None -60 2 Rat 4.8 pKd = 4.8 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 446 8 0 5 4.0 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCc1ccc2ccccc2c1 10.1016/j.bmcl.2009.01.072
CHEMBL460934 176232 0 None -60 2 Rat 4.8 pKd = 4.8 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 446 8 0 5 4.0 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCc1ccc2ccccc2c1 10.1016/j.bmcl.2009.01.072
44441909 93773 0 None -10 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 462 4 1 5 2.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(N)=O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL249892 93773 0 None -10 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 462 4 1 5 2.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(N)=O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441916 154219 0 None -5888 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 462 3 0 5 3.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(F)c4C#N)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL400136 154219 0 None -5888 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 462 3 0 5 3.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(F)c4C#N)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441663 94042 0 None -660 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 534 4 0 7 3.9 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(cccc3OC(=O)C(C)(C)C)C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL251529 94042 0 None -660 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 534 4 0 7 3.9 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(cccc3OC(=O)C(C)(C)C)C[C@H]21 10.1016/j.bmcl.2007.04.086
44447011 94344 0 None -3715 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 493 2 1 4 3.6 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL253438 94344 0 None -3715 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 493 2 1 4 3.6 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44441867 93797 0 None -9 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 420 3 0 5 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccncc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250111 93797 0 None -9 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 420 3 0 5 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccncc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44447023 94096 0 None -6 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 477 3 1 5 2.6 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c([S+](C)[O-])c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL251801 94096 0 None -6 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 477 3 1 5 2.6 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c([S+](C)[O-])c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44447006 94315 0 None -1258 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 415 2 1 4 2.9 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL253232 94315 0 None -1258 2 Rat 4.8 pKd = 4.8 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 415 2 1 4 2.9 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44564815 189150 0 None -1905 2 Rat 5.7 pKd = 5.7 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 498 9 0 5 5.2 CCN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL515907 189150 0 None -1905 2 Rat 5.7 pKd = 5.7 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 498 9 0 5 5.2 CCN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44564744 176359 0 None -630 2 Rat 4.7 pKd = 4.7 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 498 8 0 5 4.7 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2Cc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL462159 176359 0 None -630 2 Rat 4.7 pKd = 4.7 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 498 8 0 5 4.7 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2Cc2ccccc21 10.1016/j.bmcl.2009.01.072
44441890 94013 0 None -1047 2 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 437 3 0 4 3.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccc4F)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL251311 94013 0 None -1047 2 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 437 3 0 4 3.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccc4F)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441672 94084 0 None -3311 2 Rat 5.7 pKd = 5.7 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 618 5 0 10 3.5 Cc1ccc(S(=O)(=O)Oc2cccc3c2C[C@H]2C[C@@H](C(=O)N4CCN(c5ccc6nsnc6n5)CC4)CN(C)[C@@H]2C3)cc1 10.1016/j.bmcl.2007.04.086
CHEMBL251753 94084 0 None -3311 2 Rat 5.7 pKd = 5.7 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 618 5 0 10 3.5 Cc1ccc(S(=O)(=O)Oc2cccc3c2C[C@H]2C[C@@H](C(=O)N4CCN(c5ccc6nsnc6n5)CC4)CN(C)[C@@H]2C3)cc1 10.1016/j.bmcl.2007.04.086
10162564 12418 0 None -33884 8 Rat 4.7 pKd = 4.7 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 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 12418 0 None -33884 8 Rat 4.7 pKd = 4.7 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 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 12418 0 None -33884 8 Rat 4.7 pKd = 4.7 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 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
9849682 94498 0 None -95499 10 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
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 94498 0 None -95499 10 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
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
44447060 193153 0 None -363 2 Rat 5.7 pKd = 5.7 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 526 2 1 3 4.9 CN1C[C@H](C(=O)N2CCN(c3ccc(Cl)cc3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL539415 193153 0 None -363 2 Rat 5.7 pKd = 5.7 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 526 2 1 3 4.9 CN1C[C@H](C(=O)N2CCN(c3ccc(Cl)cc3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44441910 93774 0 None -11 2 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 518 6 0 5 3.6 CCN(CC)C(=O)c1ccc(N2CCN(C(=O)[C@@H]3C[C@@H]4Cc5c(cccc5OC)C[C@H]4N(C)C3)CC2)cc1 10.1016/j.bmcl.2007.04.078
CHEMBL249893 93774 0 None -11 2 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 518 6 0 5 3.6 CCN(CC)C(=O)c1ccc(N2CCN(C(=O)[C@@H]3C[C@@H]4Cc5c(cccc5OC)C[C@H]4N(C)C3)CC2)cc1 10.1016/j.bmcl.2007.04.078
44441871 93821 0 None -190 2 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 488 3 0 5 3.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(F)(F)F)cn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250313 93821 0 None -190 2 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 488 3 0 5 3.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(F)(F)F)cn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL2370167 208051 0 None 45 5 Human 8.7 pKd = 8.7 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst2) expressed in CHO cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst2) 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
CHEMBL5089315 213761 0 None - 1 Mouse 8.6 pKd = 8.6 Binding
Binding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysisBinding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01791
CHEMBL5095828 213761 0 None - 1 Mouse 8.6 pKd = 8.6 Binding
Binding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysisBinding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01791
CHEMBL5078027 213756 0 None - 1 Mouse 8.5 pKd = 8.5 Binding
Binding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysisBinding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01791
CHEMBL5095771 213756 0 None - 1 Mouse 8.5 pKd = 8.5 Binding
Binding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysisBinding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01791
CHEMBL2370168 208052 0 None 18 5 Human 8.5 pKd = 8.5 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst2) expressed in CHO cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst2) 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
44441928 93977 0 None -4 2 Rat 5.7 pKd = 5.7 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 474 3 1 5 3.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCC(n4c(=O)[nH]c5ccccc54)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL251111 93977 0 None -4 2 Rat 5.7 pKd = 5.7 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 474 3 1 5 3.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCC(n4c(=O)[nH]c5ccccc54)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44447077 94166 0 None -48 7 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
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 94166 0 None -48 7 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
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
44441879 93907 0 None -75 2 Rat 5.7 pKd = 5.7 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 470 3 0 5 3.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5ccccc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250724 93907 0 None -75 2 Rat 5.7 pKd = 5.7 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 470 3 0 5 3.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5ccccc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
46880588 14087 0 None -28 7 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST2 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST2 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 14087 0 None -28 7 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST2 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST2 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 14087 0 None -28 7 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST2 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST2 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
44441887 93980 0 None -239 2 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 460 3 0 7 2.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nccn5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL251121 93980 0 None -239 2 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 460 3 0 7 2.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nccn5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441893 93746 0 None -6456 2 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 437 3 0 4 3.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(F)c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL249723 93746 0 None -6456 2 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 437 3 0 4 3.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(F)c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44447052 154400 0 None -112 2 Rat 5.7 pKd = 5.7 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 448 2 1 3 4.1 CN1C[C@H](C(=O)N2CCN(c3ccc(Cl)cc3)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL401130 154400 0 None -112 2 Rat 5.7 pKd = 5.7 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 448 2 1 3 4.1 CN1C[C@H](C(=O)N2CCN(c3ccc(Cl)cc3)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44441923 93904 0 None -85 2 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 478 4 0 6 3.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250715 93904 0 None -85 2 Rat 4.7 pKd = 4.7 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 478 4 0 6 3.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
46865535 5449 0 None -67 7 Rat 6.6 pKd = 6.6 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST2 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST2 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 5449 0 None -67 7 Rat 6.6 pKd = 6.6 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST2 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST2 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
CHEMBL407209 210890 1 None -38 4 Human 7.6 pKd = 7.6 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)
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)[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/jm000361p
44441926 93941 0 None -77 2 Rat 5.6 pKd = 5.6 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 417 3 0 4 3.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CC=C(c4ccccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250914 93941 0 None -77 2 Rat 5.6 pKd = 5.6 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 417 3 0 4 3.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CC=C(c4ccccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441927 93976 0 None -4 2 Rat 5.6 pKd = 5.6 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 418 3 0 5 2.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CC=C(c4ncccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL251110 93976 0 None -4 2 Rat 5.6 pKd = 5.6 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 418 3 0 5 2.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CC=C(c4ncccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441905 93901 0 None -38 2 Rat 4.6 pKd = 4.6 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 435 3 1 5 2.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250704 93901 0 None -38 2 Rat 4.6 pKd = 4.6 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 435 3 1 5 2.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441924 93940 0 None -30 2 Rat 5.6 pKd = 5.6 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 450 3 0 3 4.7 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CC=C(c4ccc(Cl)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250912 93940 0 None -30 2 Rat 5.6 pKd = 5.6 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 450 3 0 3 4.7 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CC=C(c4ccc(Cl)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441868 154290 0 None -478 2 Rat 4.6 pKd = 4.6 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 421 3 0 6 1.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccnn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL400481 154290 0 None -478 2 Rat 4.6 pKd = 4.6 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 421 3 0 6 1.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccnn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL413830 211331 0 None 2 5 Human 7.6 pKd = 7.6 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)
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
44441894 154360 0 None -7762 2 Rat 4.6 pKd = 4.6 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 437 3 0 4 3.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(F)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL400907 154360 0 None -7762 2 Rat 4.6 pKd = 4.6 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 437 3 0 4 3.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(F)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44447049 94500 0 None -93325 2 Rat 4.6 pKd = 4.6 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 537 3 1 5 3.4 CCn1c(N2CCN(C(=O)[C@@H]3C[C@@H]4c5cccc6[nH]c(Br)c(c56)C[C@H]4N(C)C3)CC2)cccc1=O 10.1016/j.bmcl.2007.12.030
CHEMBL254505 94500 0 None -93325 2 Rat 4.6 pKd = 4.6 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 537 3 1 5 3.4 CCn1c(N2CCN(C(=O)[C@@H]3C[C@@H]4c5cccc6[nH]c(Br)c(c56)C[C@H]4N(C)C3)CC2)cccc1=O 10.1016/j.bmcl.2007.12.030
44441869 154319 0 None -58 2 Rat 4.6 pKd = 4.6 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 421 3 0 6 1.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ncccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL400677 154319 0 None -58 2 Rat 4.6 pKd = 4.6 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 421 3 0 6 1.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ncccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441679 93645 0 None -83 2 Rat 5.5 pKd = 5.5 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 520 4 0 9 2.7 COc1ccc(C(C)=O)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL249111 93645 0 None -83 2 Rat 5.5 pKd = 5.5 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 520 4 0 9 2.7 COc1ccc(C(C)=O)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL5087925 213770 0 None - 1 Mouse 8.4 pKd = 8.4 Binding
Binding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysisBinding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01791
CHEMBL5095894 213770 0 None - 1 Mouse 8.4 pKd = 8.4 Binding
Binding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysisBinding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01791
44447074 94102 0 None -2951 2 Rat 5.5 pKd = 5.5 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 473 2 1 7 2.9 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL251836 94102 0 None -2951 2 Rat 5.5 pKd = 5.5 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 473 2 1 7 2.9 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44447062 94132 0 None -812 2 Rat 5.5 pKd = 5.5 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 459 3 1 5 3.4 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252029 94132 0 None -812 2 Rat 5.5 pKd = 5.5 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 459 3 1 5 3.4 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44441660 94016 0 None -204 2 Rat 4.5 pKd = 4.5 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 390 2 0 4 2.5 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2Cc3ccccc3C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL251335 94016 0 None -204 2 Rat 4.5 pKd = 4.5 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 390 2 0 4 2.5 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2Cc3ccccc3C[C@H]21 10.1016/j.bmcl.2007.04.086
44564702 189266 0 None -190 2 Rat 5.5 pKd = 5.5 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 512 8 0 5 4.9 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2CCc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL516837 189266 0 None -190 2 Rat 5.5 pKd = 5.5 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 512 8 0 5 4.9 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2CCc2ccccc21 10.1016/j.bmcl.2009.01.072
44441884 93944 0 None -2041 2 Rat 5.5 pKd = 5.5 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 461 3 0 7 2.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nonc5c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250922 93944 0 None -2041 2 Rat 5.5 pKd = 5.5 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 461 3 0 7 2.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nonc5c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441921 93903 0 None -165 2 Rat 4.5 pKd = 4.5 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 434 3 0 5 2.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCCN(c4ccccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250713 93903 0 None -165 2 Rat 4.5 pKd = 4.5 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 434 3 0 5 2.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCCN(c4ccccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
46865536 11799 0 None -457 7 Human 5.5 pKd = 5.5 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 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 11799 0 None -457 7 Human 5.5 pKd = 5.5 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 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 11799 0 None -457 7 Human 5.5 pKd = 5.5 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 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
44441666 154170 0 None -2290 2 Rat 5.5 pKd = 5.5 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 582 5 0 8 3.2 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(cccc3OS(=O)(=O)C(F)(F)F)C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL399843 154170 0 None -2290 2 Rat 5.5 pKd = 5.5 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 582 5 0 8 3.2 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(cccc3OS(=O)(=O)C(F)(F)F)C[C@H]21 10.1016/j.bmcl.2007.04.086
44441883 93943 0 None -999 2 Rat 5.4 pKd = 5.4 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 461 3 0 7 2.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc5nonc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250921 93943 0 None -999 2 Rat 5.4 pKd = 5.4 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 461 3 0 7 2.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc5nonc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
2030 3602 7 None -51286 10 Human 4.4 pKd = 4.4 Binding
Binding affinity to human recombinant sst2 receptorBinding affinity to human recombinant sst2 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 3602 7 None -51286 10 Human 4.4 pKd = 4.4 Binding
Binding affinity to human recombinant sst2 receptorBinding affinity to human recombinant sst2 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 3602 7 None -51286 10 Human 4.4 pKd = 4.4 Binding
Binding affinity to human recombinant sst2 receptorBinding affinity to human recombinant sst2 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
44441665 168556 0 None -9120 2 Rat 5.4 pKd = 5.4 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 528 5 0 8 2.3 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(cccc3OS(C)(=O)=O)C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL440236 168556 0 None -9120 2 Rat 5.4 pKd = 5.4 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 528 5 0 8 2.3 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(cccc3OS(C)(=O)=O)C[C@H]21 10.1016/j.bmcl.2007.04.086
46880588 14087 0 None -52 7 Human 4.4 pKd = 4.4 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 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 14087 0 None -52 7 Human 4.4 pKd = 4.4 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 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 14087 0 None -52 7 Human 4.4 pKd = 4.4 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 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
44447078 94167 0 None -21 7 Human 5.4 pKd = 5.4 Binding
Binding affinity to human recombinant sst2 receptorBinding affinity to human recombinant sst2 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 94167 0 None -21 7 Human 5.4 pKd = 5.4 Binding
Binding affinity to human recombinant sst2 receptorBinding affinity to human recombinant sst2 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
44441673 94085 0 None -9772 2 Rat 5.4 pKd = 5.4 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 596 4 0 10 2.7 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2Cc3c(cccc3OS(=O)(=O)C(F)(F)F)C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL251754 94085 0 None -9772 2 Rat 5.4 pKd = 5.4 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 596 4 0 10 2.7 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2Cc3c(cccc3OS(=O)(=O)C(F)(F)F)C[C@H]21 10.1016/j.bmcl.2007.04.086
44447075 94135 0 None -16218 2 Rat 5.4 pKd = 5.4 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 507 2 1 7 3.5 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252032 94135 0 None -16218 2 Rat 5.4 pKd = 5.4 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 507 2 1 7 3.5 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL5078119 213757 0 None - 1 Mouse 8.3 pKd = 8.3 Binding
Binding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysisBinding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01791
CHEMBL5095772 213757 0 None - 1 Mouse 8.3 pKd = 8.3 Binding
Binding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysisBinding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01791
CHEMBL386676 210629 0 None 2 4 Human 7.4 pKd = 7.4 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)
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)[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/jm000361p
44564856 179082 0 None -575 2 Rat 5.4 pKd = 5.4 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 510 10 0 5 5.3 C=CCN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL474345 179082 0 None -575 2 Rat 5.4 pKd = 5.4 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 510 10 0 5 5.3 C=CCN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44565112 12635 0 None -5623 6 Human 5.4 pKd = 5.4 Binding
Binding affinity to human sst2 receptorBinding affinity to human sst2 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1187847 12635 0 None -5623 6 Human 5.4 pKd = 5.4 Binding
Binding affinity to human sst2 receptorBinding affinity to human sst2 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL523814 12635 0 None -5623 6 Human 5.4 pKd = 5.4 Binding
Binding affinity to human sst2 receptorBinding affinity to human sst2 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44565112 12635 0 None -5623 6 Rat 5.4 pKd = 5.4 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1187847 12635 0 None -5623 6 Rat 5.4 pKd = 5.4 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL523814 12635 0 None -5623 6 Rat 5.4 pKd = 5.4 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44441886 154212 0 None -398 2 Rat 5.4 pKd = 5.4 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 477 3 0 7 3.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL400099 154212 0 None -398 2 Rat 5.4 pKd = 5.4 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 477 3 0 7 3.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441917 93818 0 None -1348 2 Rat 5.4 pKd = 5.4 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 489 4 0 7 2.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4C#N)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250305 93818 0 None -1348 2 Rat 5.4 pKd = 5.4 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 489 4 0 7 2.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4C#N)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441932 94012 0 None -4 2 Rat 4.4 pKd = 4.4 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 343 2 1 4 1.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCNCC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL251301 94012 0 None -4 2 Rat 4.4 pKd = 4.4 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 343 2 1 4 1.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCNCC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
9871544 14086 1 None -933 11 Human 5.3 pKd = 5.3 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 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 14086 1 None -933 11 Human 5.3 pKd = 5.3 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 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 14086 1 None -933 11 Human 5.3 pKd = 5.3 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 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
44447076 94136 0 None -12302 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 551 2 1 7 3.6 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252033 94136 0 None -12302 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 551 2 1 7 3.6 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44441670 154095 0 None -3981 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 554 5 0 8 4.0 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2Cc3c(cccc3OCc3ccccc3)C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL399464 154095 0 None -3981 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 554 5 0 8 4.0 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2Cc3c(cccc3OCc3ccccc3)C[C@H]21 10.1016/j.bmcl.2007.04.086
44441918 166307 0 None -44 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 532 4 0 6 4.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(F)(F)F)cc4[N+](=O)[O-])CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL428583 166307 0 None -44 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 532 4 0 6 4.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(F)(F)F)cc4[N+](=O)[O-])CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44447045 94497 0 None -125892 2 Rat 4.3 pKd = 4.3 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 479 2 1 5 2.8 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL254499 94497 0 None -125892 2 Rat 4.3 pKd = 4.3 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 479 2 1 5 2.8 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44564703 189893 0 None -446 2 Rat 5.3 pKd = 5.3 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 510 8 0 5 5.3 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2C=Cc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL517921 189893 0 None -446 2 Rat 5.3 pKd = 5.3 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 510 8 0 5 5.3 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2C=Cc2ccccc21 10.1016/j.bmcl.2009.01.072
44441903 93900 0 None -18 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 487 3 0 4 4.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(F)(F)F)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250703 93900 0 None -18 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 487 3 0 4 4.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(F)(F)F)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441671 154433 0 None -23988 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 542 4 0 10 1.8 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2Cc3c(cccc3OS(C)(=O)=O)C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL401290 154433 0 None -23988 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 542 4 0 10 1.8 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2Cc3c(cccc3OS(C)(=O)=O)C[C@H]21 10.1016/j.bmcl.2007.04.086
44447071 153578 0 None -13182 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 490 2 1 6 3.7 CN1C[C@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL398526 153578 0 None -13182 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 490 2 1 6 3.7 CN1C[C@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44441877 93856 0 None -602 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 494 3 0 5 4.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc5ccc(C#N)cc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250522 93856 0 None -602 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 494 3 0 5 4.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc5ccc(C#N)cc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441878 93906 0 None -7 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 484 3 0 5 3.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cc(C)nc5ccccc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250723 93906 0 None -7 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 484 3 0 5 3.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cc(C)nc5ccccc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441919 154220 0 None -3019 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 542 5 0 8 2.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4S(C)(=O)=O)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL400137 154220 0 None -3019 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 542 5 0 8 2.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4S(C)(=O)=O)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
46865535 5449 0 None -1621 7 Human 5.3 pKd = 5.3 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 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 5449 0 None -1621 7 Human 5.3 pKd = 5.3 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 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
44441876 93855 0 None -63 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 469 3 0 4 4.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc5ccccc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250521 93855 0 None -63 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 469 3 0 4 4.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc5ccccc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441880 168650 0 None -19 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 470 3 0 5 3.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cc5ccccc5cn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL440962 168650 0 None -19 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 470 3 0 5 3.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cc5ccccc5cn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL384836 210580 0 None -3 5 Human 7.3 pKd = 7.3 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)
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
CHEMBL409019 210985 0 None -1 5 Human 7.3 pKd = 7.3 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)
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
44447014 94375 0 None -338 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 541 2 1 4 3.5 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(I)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL253653 94375 0 None -338 2 Rat 5.3 pKd = 5.3 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 541 2 1 4 3.5 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(I)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44441669 93567 0 None -4677 2 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 478 3 0 8 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL248715 93567 0 None -4677 2 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 478 3 0 8 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441669 93567 0 None -4677 2 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 478 3 0 8 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL248715 93567 0 None -4677 2 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 478 3 0 8 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
44441661 94043 0 None -7079 2 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 492 5 0 6 3.8 CC(C)Oc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL251542 94043 0 None -7079 2 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 492 5 0 6 3.8 CC(C)Oc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
44447058 154401 0 None -1412 2 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 482 2 1 3 4.8 CN1C[C@H](C(=O)N2CCN(c3ccc(Cl)cc3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL401131 154401 0 None -1412 2 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 482 2 1 3 4.8 CN1C[C@H](C(=O)N2CCN(c3ccc(Cl)cc3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL2370166 208050 0 None 7 5 Human 8.2 pKd = 8.2 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst2) expressed in CHO cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst2) 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
CHEMBL5087277 213782 0 None - 1 Mouse 8.2 pKd = 8.2 Binding
Binding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysisBinding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01791
CHEMBL5096010 213782 0 None - 1 Mouse 8.2 pKd = 8.2 Binding
Binding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysisBinding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01791
44564745 176376 0 None -478 2 Rat 5.2 pKd = 5.2 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 516 8 0 6 5.3 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL462335 176376 0 None -478 2 Rat 5.2 pKd = 5.2 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 516 8 0 6 5.3 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL437093 211947 0 None 1 5 Human 7.2 pKd = 7.2 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)
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
44441930 94011 0 None -87 2 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 429 2 1 3 3.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCc4c([nH]c5ccccc45)C3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL251300 94011 0 None -87 2 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 429 2 1 3 3.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCc4c([nH]c5ccccc45)C3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441677 93604 0 None -5248 2 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 556 3 0 8 3.2 COc1ccc(Br)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL248907 93604 0 None -5248 2 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 556 3 0 8 3.2 COc1ccc(Br)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
17955460 176191 0 None -8317 9 Rat 5.2 pKd = 5.2 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 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 176191 0 None -8317 9 Rat 5.2 pKd = 5.2 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 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
44447073 94101 0 None -17378 10 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
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 94101 0 None -17378 10 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
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
44441873 93978 0 None -63 2 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 526 6 0 6 4.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(OCc5ccccc5)n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL251116 93978 0 None -63 2 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 526 6 0 6 4.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(OCc5ccccc5)n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44447073 94101 0 None -18197 10 Human 5.2 pKd = 5.2 Binding
Binding affinity to human recombinant sst2 receptorBinding affinity to human recombinant sst2 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 94101 0 None -18197 10 Human 5.2 pKd = 5.2 Binding
Binding affinity to human recombinant sst2 receptorBinding affinity to human recombinant sst2 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
44564746 176377 0 None -7585 2 Rat 5.2 pKd = 5.2 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 500 8 0 6 4.9 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL462336 176377 0 None -7585 2 Rat 5.2 pKd = 5.2 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 500 8 0 6 4.9 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
44441900 93851 0 None -5128 2 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc([N+](=O)[O-])c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250498 93851 0 None -5128 2 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc([N+](=O)[O-])c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
17955460 176191 0 None -8912 9 Human 5.2 pKd = 5.2 Binding
Binding affinity to human sst2 receptorBinding affinity to human sst2 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 176191 0 None -8912 9 Human 5.2 pKd = 5.2 Binding
Binding affinity to human sst2 receptorBinding affinity to human sst2 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
44564783 176341 0 None -9772 4 Rat 5.2 pKd = 5.2 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 484 8 0 5 4.8 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL461988 176341 0 None -9772 4 Rat 5.2 pKd = 5.2 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 484 8 0 5 4.8 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44564857 178350 0 None -151 4 Rat 5.2 pKd = 5.2 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 524 10 0 5 5.5 O=C(CCN(CCC1c2ccccc2-c2ccccc21)CC1CC1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.bmcl.2009.01.072
CHEMBL470331 178350 0 None -151 4 Rat 5.2 pKd = 5.2 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 524 10 0 5 5.5 O=C(CCN(CCC1c2ccccc2-c2ccccc21)CC1CC1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.bmcl.2009.01.072
44441882 93942 0 None -19 2 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 472 3 0 7 2.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cc5nccnc5cn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250920 93942 0 None -19 2 Rat 5.2 pKd = 5.2 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 472 3 0 7 2.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cc5nccnc5cn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441668 94083 0 None -1202 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 476 4 0 6 3.2 CC(=O)c1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL251752 94083 0 None -1202 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 476 4 0 6 3.2 CC(=O)c1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
44441667 154390 0 None -457 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 459 3 0 6 2.9 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(C#N)cccc3C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL401091 154390 0 None -457 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 459 3 0 6 2.9 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(C#N)cccc3C[C@H]21 10.1016/j.bmcl.2007.04.086
44447066 94163 0 None -5370 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 537 3 1 5 4.1 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252229 94163 0 None -5370 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 537 3 1 5 4.1 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44441897 93775 0 None -3715 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 444 3 0 5 3.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccc4C#N)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL249930 93775 0 None -3715 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 444 3 0 5 3.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccc4C#N)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
2030 3602 7 None -10964 10 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
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.2007.04.078
5311377 3602 7 None -10964 10 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
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.2007.04.078
CHEMBL251541 3602 7 None -10964 10 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
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.2007.04.078
2030 3602 7 None -10964 10 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
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 3602 7 None -10964 10 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
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 3602 7 None -10964 10 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
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
44441662 94044 0 None -416 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 450 3 1 6 2.7 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL251543 94044 0 None -416 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 450 3 1 6 2.7 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmcl.2007.04.086
44447043 94469 0 None -10232 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 445 2 1 5 2.2 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL254288 94469 0 None -10232 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 445 2 1 5 2.2 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44447025 154396 0 None -25 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 493 3 1 6 2.3 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(S(C)(=O)=O)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL401108 154396 0 None -25 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 493 3 1 6 2.3 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(S(C)(=O)=O)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44447026 94131 0 None -46 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 479 2 2 4 3.3 O=C([C@H]1CN[C@@H]2Cc3c(Br)[nH]c4cccc(c34)[C@H]2C1)N1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2007.12.030
CHEMBL252002 94131 0 None -46 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 479 2 2 4 3.3 O=C([C@H]1CN[C@@H]2Cc3c(Br)[nH]c4cccc(c34)[C@H]2C1)N1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2007.12.030
CHEMBL5086057 213780 0 None - 1 Mouse 8.1 pKd = 8.1 Binding
Binding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysisBinding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01791
CHEMBL5095976 213780 0 None - 1 Mouse 8.1 pKd = 8.1 Binding
Binding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysisBinding affinity to mouse SST2 expressed in mouse pheochromocytoma cells assessed as dissociation constant for 1 hr by nanodrop spectrophotometric analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01791
CHEMBL405561 210809 0 None -3 4 Human 8.1 pKd = 8.1 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](N(C)C(=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)N1)C(N)=O 10.1021/jm000361p
44565159 193212 0 None -25118 5 Rat 5.1 pKd = 5.1 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 497 7 0 7 4.5 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL540705 193212 0 None -25118 5 Rat 5.1 pKd = 5.1 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 497 7 0 7 4.5 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
44447038 94222 0 None -16595 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 528 2 1 3 4.5 CN1C[C@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252618 94222 0 None -16595 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 528 2 1 3 4.5 CN1C[C@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44564814 179447 0 None -602 2 Rat 5.1 pKd = 5.1 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 486 10 0 5 4.8 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.01.072
CHEMBL474752 179447 0 None -602 2 Rat 5.1 pKd = 5.1 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 486 10 0 5 4.8 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.01.072
44447016 94376 0 None -35 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 431 2 2 5 2.6 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(O)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL253654 94376 0 None -35 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 431 2 2 5 2.6 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(O)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44447019 94411 0 None -3548 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 461 3 1 5 3.6 CSc1[nH]c2cccc3c2c1C[C@@H]1[C@@H]3C[C@@H](C(=O)N2CCN(c3ccccn3)CC2)CN1C 10.1016/j.bmcl.2007.12.030
CHEMBL253879 94411 0 None -3548 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 461 3 1 5 3.6 CSc1[nH]c2cccc3c2c1C[C@@H]1[C@@H]3C[C@@H](C(=O)N2CCN(c3ccccn3)CC2)CN1C 10.1016/j.bmcl.2007.12.030
44564785 176358 0 None -112 2 Rat 5.1 pKd = 5.1 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 446 8 0 5 4.0 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCc1cccc2ccccc12 10.1016/j.bmcl.2009.01.072
CHEMBL462158 176358 0 None -112 2 Rat 5.1 pKd = 5.1 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 446 8 0 5 4.0 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCc1cccc2ccccc12 10.1016/j.bmcl.2009.01.072
44441913 93796 0 None -13 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 497 4 0 6 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(S(C)(=O)=O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250098 93796 0 None -13 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 497 4 0 6 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(S(C)(=O)=O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441906 93902 0 None -57 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 461 4 0 5 3.3 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(C)=O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250705 93902 0 None -57 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 461 4 0 5 3.3 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(C)=O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44447064 153824 0 None -7079 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 493 3 1 5 4.0 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL398712 153824 0 None -7079 2 Rat 5.1 pKd = 5.1 Binding
Displacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortexDisplacement of [125I][Tyr3]octreotide from sst2 receptor in rat cortex
ChEMBL 493 3 1 5 4.0 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL413373 211304 0 None -3 4 Human 8.0 pKd = 8.0 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst2)
ChEMBL None None None CN[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)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](Cc2ccccc2)NC1=O 10.1021/jm000361p
44564816 188912 0 None -194 2 Rat 6.0 pKd = 6.0 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 512 9 0 5 5.5 CC(C)N(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL514027 188912 0 None -194 2 Rat 6.0 pKd = 6.0 Binding
Binding affinity to rat sst2 receptorBinding affinity to rat sst2 receptor
ChEMBL 512 9 0 5 5.5 CC(C)N(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44441914 153357 0 None -15 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 498 4 1 6 1.7 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(S(N)(=O)=O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL398319 153357 0 None -15 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 498 4 1 6 1.7 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(S(N)(=O)=O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441931 154272 0 None -19 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 433 4 0 4 3.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(Cc4ccccc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL400386 154272 0 None -19 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL 433 4 0 4 3.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(Cc4ccccc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441675 93568 0 None -1995 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 542 4 0 6 3.8 COc1ccc(Br)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL248716 93568 0 None -1995 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
ChEMBL 542 4 0 6 3.8 COc1ccc(Br)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
44447077 94166 0 None -22 7 Human 5.0 pKd = 5.0 Binding
Binding affinity to human recombinant sst2 receptorBinding affinity to human recombinant sst2 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 94166 0 None -22 7 Human 5.0 pKd = 5.0 Binding
Binding affinity to human recombinant sst2 receptorBinding affinity to human recombinant sst2 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
15965425 2167 4 None 3090 5 Human 11.0 pKi = 11 Binding
Binding affinity towards Somatostatin receptor type 2 (hsst2)Binding affinity towards Somatostatin receptor type 2 (hsst2)
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 2167 4 None 3090 5 Human 11.0 pKi = 11 Binding
Binding affinity towards Somatostatin receptor type 2 (hsst2)Binding affinity towards Somatostatin receptor type 2 (hsst2)
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 2167 4 None 3090 5 Human 11.0 pKi = 11 Binding
Binding affinity towards Somatostatin receptor type 2 (hsst2)Binding affinity towards Somatostatin receptor type 2 (hsst2)
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
15965425 2167 4 None 3090 5 Human 11.0 pKi = 11 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing each of the cloned human SRIF receptor (sst-2) subtypesInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing each of the cloned human SRIF receptor (sst-2) subtypes
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/jm0108449
2046 2167 4 None 3090 5 Human 11.0 pKi = 11 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing each of the cloned human SRIF receptor (sst-2) subtypesInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing each of the cloned human SRIF receptor (sst-2) subtypes
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/jm0108449
CHEMBL99895 2167 4 None 3090 5 Human 11.0 pKi = 11 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing each of the cloned human SRIF receptor (sst-2) subtypesInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing each of the cloned human SRIF receptor (sst-2) subtypes
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/jm0108449
155567788 175463 0 None - 1 Human 10.9 pKi = 10.9 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1786 27 15 26 3.9 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(=O)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
CHEMBL4590517 175463 0 None - 1 Human 10.9 pKi = 10.9 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1786 27 15 26 3.9 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(=O)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
155551297 173370 0 None - 1 Human 10.8 pKi = 10.8 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1858 31 16 27 4.3 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSCCCN[C@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccc(O)cc3)NC1=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
CHEMBL4541310 173370 0 None - 1 Human 10.8 pKi = 10.8 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1858 31 16 27 4.3 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSCCCN[C@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccc(O)cc3)NC1=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
155554925 173740 0 None - 1 Human 10.8 pKi = 10.8 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1860 30 16 28 3.7 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSCCOc1ccc(C[C@@H](N)C(=O)N[C@H]3CSSC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](Cc4ccc(O)cc4)NC3=O)cc1)[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
CHEMBL4550617 173740 0 None - 1 Human 10.8 pKi = 10.8 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1860 30 16 28 3.7 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSCCOc1ccc(C[C@@H](N)C(=O)N[C@H]3CSSC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](Cc4ccc(O)cc4)NC3=O)cc1)[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
155562010 175239 0 None - 1 Human 10.8 pKi = 10.8 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1813 27 15 26 4.1 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSC(C)(C)[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
CHEMBL4584764 175239 0 None - 1 Human 10.8 pKi = 10.8 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1813 27 15 26 4.1 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSC(C)(C)[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
155560117 174336 0 None - 1 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1772 27 15 26 3.8 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSC[C@@H](CO)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@@]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
CHEMBL4564727 174336 0 None - 1 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1772 27 15 26 3.8 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSC[C@@H](CO)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@@]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
91809292 125233 0 None 3 4 Human 10.7 pKi = 10.7 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 1619 27 18 17 2.6 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)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647691 125233 0 None 3 4 Human 10.7 pKi = 10.7 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 1619 27 18 17 2.6 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)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
91809296 125237 0 None 16 4 Human 10.7 pKi = 10.7 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 1488 23 17 17 1.5 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](NCCS(=O)(=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
CHEMBL3647695 125237 0 None 16 4 Human 10.7 pKi = 10.7 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 1488 23 17 17 1.5 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](NCCS(=O)(=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
91809297 125238 0 None - 1 Human 10.7 pKi = 10.7 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 1635 27 18 18 2.2 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)CS(=O)(=O)C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647696 125238 0 None - 1 Human 10.7 pKi = 10.7 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 1635 27 18 18 2.2 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)CS(=O)(=O)C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
155544425 172800 0 None 436 5 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 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 172800 0 None 436 5 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 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
52936833 60903 0 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 474 6 1 5 6.5 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cnn(C)c4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766100 60903 0 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 474 6 1 5 6.5 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cnn(C)c4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
52936725 60906 19 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 432 6 2 4 6.3 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccc(O)c4)cc3c2OCCCN)c1 10.1021/jm101501b
CHEMBL1766103 60906 19 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 432 6 2 4 6.3 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccc(O)c4)cc3c2OCCCN)c1 10.1021/jm101501b
CHEMBL4299281 211800 0 None 44 2 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]tyr11-SRIF from human sst2 receptor after 60 mins by liquid scintillation counting methodDisplacement of [125I]tyr11-SRIF from human sst2 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
16129706 207277 36 None 4 5 Human 10.5 pKi = 10.5 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-2) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-2) 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 207277 36 None 4 5 Human 10.5 pKi = 10.5 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-2) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-2) 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
24951598 60900 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 486 6 2 4 7.5 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccc(O)c4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766097 60900 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 486 6 2 4 7.5 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccc(O)c4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
24951597 60902 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 513 7 2 4 6.8 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(C(N)=O)cc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766099 60902 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 513 7 2 4 6.8 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(C(N)=O)cc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
16129706 207277 36 None 4 5 Human 10.4 pKi = 10.4 Binding
Binding affinity towards Somatostatin receptor type 2 (hsst2)Binding affinity towards Somatostatin receptor type 2 (hsst2)
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 207277 36 None 4 5 Human 10.4 pKi = 10.4 Binding
Binding affinity towards Somatostatin receptor type 2 (hsst2)Binding affinity towards Somatostatin receptor type 2 (hsst2)
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 210953 0 None 9 5 Human 10.4 pKi = 10.4 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 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
91809272 125215 0 None 269 2 Human 10.4 pKi = 10.4 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 1425 22 16 13 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](NCCC[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
CHEMBL3647673 125215 0 None 269 2 Human 10.4 pKi = 10.4 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 1425 22 16 13 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](NCCC[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
91809290 125231 0 None 5 4 Human 10.4 pKi = 10.4 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 1636 27 18 16 3.3 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)C[S+]([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
CHEMBL3647689 125231 0 None 5 4 Human 10.4 pKi = 10.4 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 1636 27 18 16 3.3 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)C[S+]([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
91809293 125234 0 None 562 2 Human 10.4 pKi = 10.4 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 1928 34 20 20 3.5 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)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)C[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
CHEMBL3647692 125234 0 None 562 2 Human 10.4 pKi = 10.4 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 1928 34 20 20 3.5 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)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)C[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
91809305 125246 0 None 354 2 Human 10.4 pKi = 10.4 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 1645 29 18 16 4.3 CC(=O)N(CCCN[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
CHEMBL3647704 125246 0 None 354 2 Human 10.4 pKi = 10.4 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 1645 29 18 16 4.3 CC(=O)N(CCCN[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
16129706 207277 36 None 4 5 Human 10.3 pKi = 10.3 Binding
Inhibition of human sst2 receptor expressed in CHO cellsInhibition of human sst2 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 207277 36 None 4 5 Human 10.3 pKi = 10.3 Binding
Inhibition of human sst2 receptor expressed in CHO cellsInhibition of human sst2 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
91809291 125232 0 None 7 4 Human 10.3 pKi = 10.3 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 1473 23 16 14 2.9 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](NCC[S+]([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
CHEMBL3647690 125232 0 None 7 4 Human 10.3 pKi = 10.3 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 1473 23 16 14 2.9 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](NCC[S+]([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
91809301 125242 0 None 19 4 Human 10.3 pKi = 10.3 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 1470 22 17 16 2.4 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(=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
CHEMBL3647700 125242 0 None 19 4 Human 10.3 pKi = 10.3 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 1470 22 17 16 2.4 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(=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
91809287 159699 0 None 1 6 Human 10.3 pKi = 10.3 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 159699 0 None 1 6 Human 10.3 pKi = 10.3 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
13690207 114870 0 None 29 5 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]-somatostatin from human SSTR2 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR2 expressed in CHO-K1 cells
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 10.1016/j.bmcl.2013.11.065
CHEMBL3350037 114870 0 None 29 5 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]-somatostatin from human SSTR2 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR2 expressed in CHO-K1 cells
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 10.1016/j.bmcl.2013.11.065
91809288 125230 0 None 4 6 Human 10.2 pKi = 10.2 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 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 125230 0 None 4 6 Human 10.2 pKi = 10.2 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 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
155569009 175561 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1742 26 14 25 4.5 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSCCNC(=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@@]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
CHEMBL4592483 175561 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1742 26 14 25 4.5 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSCCNC(=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@@]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
54586271 60912 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 506 6 2 3 8.1 Cc1cc(C)cc(C2=C(OCCC3CCCCN3)c3cc(-c4ccc(Cl)cc4)c(Cl)cc3NC2)c1 10.1021/jm101501b
CHEMBL1766109 60912 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 506 6 2 3 8.1 Cc1cc(C)cc(C2=C(OCCC3CCCCN3)c3cc(-c4ccc(Cl)cc4)c(Cl)cc3NC2)c1 10.1021/jm101501b
155561297 175100 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1827 28 15 26 4.5 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCC(C)(C)SSC[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
CHEMBL4581874 175100 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1827 28 15 26 4.5 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCC(C)(C)SSC[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
2051 3507 20 None 2 9 Human 10.1 pKi = 10.1 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
5311430 3507 20 None 2 9 Human 10.1 pKi = 10.1 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL311695 3507 20 None 2 9 Human 10.1 pKi = 10.1 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
2054 3899 11 None 2 11 Human 10.1 pKi = 10.1 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
71306 3899 11 None 2 11 Human 10.1 pKi = 10.1 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL264186 3899 11 None 2 11 Human 10.1 pKi = 10.1 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL3349523 3899 11 None 2 11 Human 10.1 pKi = 10.1 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
DB04894 3899 11 None 2 11 Human 10.1 pKi = 10.1 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL3349516 209661 0 None 1 4 Human 10.1 pKi = 10.1 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) 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(N)=O)NC(=O)[C@H](C)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
24952323 60899 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 486 6 2 4 7.5 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(O)cc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766096 60899 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 486 6 2 4 7.5 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(O)cc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
24956953 60905 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 459 7 2 4 5.7 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccc(C(N)=O)c4)cc3c2OCCCN)c1 10.1021/jm101501b
CHEMBL1766102 60905 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 459 7 2 4 5.7 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccc(C(N)=O)c4)cc3c2OCCCN)c1 10.1021/jm101501b
91809283 125226 0 None 6 6 Human 10.1 pKi = 10.1 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 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 125226 0 None 6 6 Human 10.1 pKi = 10.1 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 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
91809294 125235 0 None 10 4 Human 10.1 pKi = 10.1 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 1912 34 19 19 3.8 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)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647693 125235 0 None 10 4 Human 10.1 pKi = 10.1 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 1912 34 19 19 3.8 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)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
91809300 125241 0 None 30 4 Human 10.1 pKi = 10.1 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 1454 22 16 15 2.7 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(=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
CHEMBL3647699 125241 0 None 30 4 Human 10.1 pKi = 10.1 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 1454 22 16 15 2.7 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(=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
16129706 207277 36 None 4 5 Human 10.1 pKi = 10.1 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
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.2005.05.061
CHEMBL1823872 207277 36 None 4 5 Human 10.1 pKi = 10.1 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
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.2005.05.061
91809299 125240 0 None 3715 2 Human 10.1 pKi = 10.1 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 1440 23 16 15 3.1 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](Cc2ccccc2)NC1=O nan
CHEMBL3647698 125240 0 None 3715 2 Human 10.1 pKi = 10.1 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 1440 23 16 15 3.1 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](Cc2ccccc2)NC1=O nan
24952682 60901 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 500 7 2 4 7.2 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(CO)cc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766098 60901 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 500 7 2 4 7.2 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(CO)cc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
155556911 173957 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1691 28 12 22 5.7 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSCCC(=O)NCCCC[C@H]1C(=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)N[C@@H](Cc3ccccc3)C(=O)N1C)[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
CHEMBL4556000 173957 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1691 28 12 22 5.7 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSCCC(=O)NCCCC[C@H]1C(=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)N[C@@H](Cc3ccccc3)C(=O)N1C)[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
24953027 60898 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 471 6 1 4 7.1 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccncc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766095 60898 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 471 6 1 4 7.1 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccncc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
24953029 60897 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 489 6 1 4 7.3 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(F)nc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766094 60897 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 489 6 1 4 7.3 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(F)nc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
155546353 172967 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1843 29 16 27 3.3 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSCCNC(=O)[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@@H](C)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
CHEMBL4532058 172967 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1843 29 16 27 3.3 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSCCNC(=O)[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@@H](C)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
155550944 173686 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1828 31 15 26 4.5 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSCCCN[C@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC1=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
CHEMBL4549303 173686 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1828 31 15 26 4.5 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSCCCN[C@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC1=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
91809275 125218 0 None 7 6 Human 9.9 pKi = 9.9 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 125218 0 None 7 6 Human 9.9 pKi = 9.9 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
CHEMBL3349521 209665 0 None 1 4 Human 9.9 pKi = 9.9 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) 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(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](C)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm021093t
52936625 60892 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 471 6 1 4 7.1 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccnc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766089 60892 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 471 6 1 4 7.1 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccnc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
52936724 60896 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 505 6 1 4 7.8 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(Cl)nc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766093 60896 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 505 6 1 4 7.8 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(Cl)nc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
52936830 60907 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 476 7 2 6 5.4 Cn1cc(-c2cc3c(OCC[C@H]4CCCCN4)c(-c4cccc(CO)c4)cnc3cc2Cl)cn1 10.1021/jm101501b
CHEMBL1766104 60907 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 476 7 2 6 5.4 Cn1cc(-c2cc3c(OCC[C@H]4CCCCN4)c(-c4cccc(CO)c4)cnc3cc2Cl)cn1 10.1021/jm101501b
52936831 60908 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 468 8 3 5 5.5 OCc1cccc(-c2ccc3ncc(-c4cccc(CO)c4)c(OCC[C@H]4CCCCN4)c3c2)c1 10.1021/jm101501b
CHEMBL1766105 60908 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 468 8 3 5 5.5 OCc1cccc(-c2ccc3ncc(-c4cccc(CO)c4)c(OCC[C@H]4CCCCN4)c3c2)c1 10.1021/jm101501b
91809285 125228 0 None 12 6 Human 9.9 pKi = 9.9 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 125228 0 None 12 6 Human 9.9 pKi = 9.9 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
91809307 125248 0 None 363 2 Human 9.9 pKi = 9.9 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 1496 24 16 14 3.4 CC(=O)N(CCCN[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)C[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 nan
CHEMBL3647706 125248 0 None 363 2 Human 9.9 pKi = 9.9 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 1496 24 16 14 3.4 CC(=O)N(CCCN[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)C[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 nan
155554285 173623 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1907 29 16 28 0.9 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSC1CC(=O)N(CC(=O)NC[C@H](NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](N)Cc4ccccc4)C(=O)N[C@@H](Cc4ccc(O)cc4)C(=O)N[C@H](Cc4c[nH]c5ccccc45)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N3)C(N)=O)C1=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
CHEMBL4548228 173623 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1907 29 16 28 0.9 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSC1CC(=O)N(CC(=O)NC[C@H](NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](N)Cc4ccccc4)C(=O)N[C@@H](Cc4ccc(O)cc4)C(=O)N[C@H](Cc4c[nH]c5ccccc45)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N3)C(N)=O)C1=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
155559238 174271 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 2551 54 20 35 3.4 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSC1CC(=O)N(CCCNC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc3ccccc3)NC(=O)CNC(=O)CCCCCN3C(=O)CC(SCCCN[C@H](Cc4ccccc4)C(=O)N[C@H]4CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc5c[nH]c6ccccc56)NC(=O)[C@H](Cc5ccccc5)NC4=O)C3=O)C1=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
CHEMBL4563111 174271 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 2551 54 20 35 3.4 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSC1CC(=O)N(CCCNC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc3ccccc3)NC(=O)CNC(=O)CCCCCN3C(=O)CC(SCCCN[C@H](Cc4ccccc4)C(=O)N[C@H]4CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc5c[nH]c6ccccc56)NC(=O)[C@H](Cc5ccccc5)NC4=O)C3=O)C1=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
91809306 125247 0 None 16 4 Human 9.9 pKi = 9.9 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 1738 28 16 17 6.7 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](N(CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647705 125247 0 None 16 4 Human 9.9 pKi = 9.9 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 1738 28 16 17 6.7 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](N(CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
91809280 125223 0 None 199 2 Human 9.8 pKi = 9.8 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](Cc2cccc(F)c2)NC1=O nan
CHEMBL3647681 125223 0 None 199 2 Human 9.8 pKi = 9.8 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](Cc2cccc(F)c2)NC1=O nan
CHEMBL3349522 209666 0 None 1 4 Human 9.8 pKi = 9.8 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None C[C@H](N)C(=O)N[C@@H](C)C(=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](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm021093t
91809295 125236 0 None - 1 Human 9.8 pKi = 9.8 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 1652 27 18 17 3.0 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)CS(=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
CHEMBL3647694 125236 0 None - 1 Human 9.8 pKi = 9.8 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 1652 27 18 17 3.0 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)CS(=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
91809286 125229 0 None -1 6 Human 9.8 pKi = 9.8 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 125229 0 None -1 6 Human 9.8 pKi = 9.8 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
91809312 125253 0 None 588 3 Human 9.8 pKi = 9.8 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 1754 28 17 18 6.4 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](N(CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCSC[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
CHEMBL3647711 125253 0 None 588 3 Human 9.8 pKi = 9.8 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 1754 28 17 18 6.4 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](N(CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCSC[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
54586272 60913 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 472 6 2 3 7.5 Cc1cc(C)cc(C2=C(OCCC3CCCCN3)c3cc(-c4ccccc4)c(Cl)cc3NC2)c1 10.1021/jm101501b
CHEMBL1766110 60913 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 472 6 2 3 7.5 Cc1cc(C)cc(C2=C(OCCC3CCCCN3)c3cc(-c4ccccc4)c(Cl)cc3NC2)c1 10.1021/jm101501b
155561497 175090 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1869 42 16 25 3.8 CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)c1ccccc1)OC)N(C)C(=O)[C@@H](NC(=O)[C@H](C(C)C)N(C)C(=O)OCCSSC[C@H](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)C(N)=O)C(C)C 10.1021/acs.jmedchem.8b02036
CHEMBL4581646 175090 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1869 42 16 25 3.8 CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)c1ccccc1)OC)N(C)C(=O)[C@@H](NC(=O)[C@H](C(C)C)N(C)C(=O)OCCSSC[C@H](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)C(N)=O)C(C)C 10.1021/acs.jmedchem.8b02036
155548259 173185 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1940 32 15 25 7.3 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSCCCN[C@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccc(O)cc3)NC1=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
CHEMBL4537192 173185 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1940 32 15 25 7.3 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSCCCN[C@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccc(O)cc3)NC1=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
16129706 207277 36 None 4 5 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) 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 207277 36 None 4 5 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) 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
CHEMBL3349600 209673 0 None 999 2 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined 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]2C[C@@H](O)CN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm021093t
16129706 207277 36 None 4 5 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 207277 36 None 4 5 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
91809284 125227 0 None 7 6 Human 9.7 pKi = 9.7 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 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 125227 0 None 7 6 Human 9.7 pKi = 9.7 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 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
16129706 207277 36 None 4 5 Human 9.6 pKi = 9.6 Binding
Binding affinity towards somatostatin receptor type 2Binding affinity towards somatostatin receptor type 2
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 207277 36 None 4 5 Human 9.6 pKi = 9.6 Binding
Binding affinity towards somatostatin receptor type 2Binding affinity towards somatostatin receptor type 2
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
91809310 125251 0 None 3 4 Human 9.6 pKi = 9.6 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 1618 27 19 17 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](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(O)cc2)NC1=O nan
CHEMBL3647709 125251 0 None 3 4 Human 9.6 pKi = 9.6 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 1618 27 19 17 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](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(O)cc2)NC1=O nan
CHEMBL1794035 207184 0 None 4 5 Human 9.6 pKi = 9.6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
91809279 125222 0 None 102 2 Human 9.6 pKi = 9.6 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 1475 23 16 14 4.0 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](Cc2cc(F)cc(F)c2)NC1=O nan
CHEMBL3647680 125222 0 None 102 2 Human 9.6 pKi = 9.6 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 1475 23 16 14 4.0 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](Cc2cc(F)cc(F)c2)NC1=O nan
91809321 125845 0 None 77 2 Human 9.6 pKi = 9.6 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 1503 24 16 15 2.9 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](NCCCS(=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
CHEMBL3650457 125845 0 None 77 2 Human 9.6 pKi = 9.6 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 1503 24 16 15 2.9 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](NCCCS(=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
155565146 174904 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1912 46 16 25 5.0 CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)c1ccccc1)OC)N(C)C(=O)[C@@H](NC(=O)[C@H](C(C)C)N(C)C(=O)OCCSSCCCN[C@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)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](Cc2ccccc2)NC1=O)C(C)C 10.1021/acs.jmedchem.8b02036
CHEMBL4577466 174904 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1912 46 16 25 5.0 CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)c1ccccc1)OC)N(C)C(=O)[C@@H](NC(=O)[C@H](C(C)C)N(C)C(=O)OCCSSCCCN[C@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)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](Cc2ccccc2)NC1=O)C(C)C 10.1021/acs.jmedchem.8b02036
52936721 60893 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 487 6 2 4 6.4 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(=O)[nH]c4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766090 60893 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 487 6 2 4 6.4 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(=O)[nH]c4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
91809308 125249 0 None 4 4 Human 9.6 pKi = 9.6 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 1602 27 18 16 4.2 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](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
CHEMBL3647707 125249 0 None 4 4 Human 9.6 pKi = 9.6 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 1602 27 18 16 4.2 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](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
2051 3507 20 None 2 9 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL None None None None 10.1021/jm980118e
5311430 3507 20 None 2 9 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL None None None None 10.1021/jm980118e
CHEMBL311695 3507 20 None 2 9 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL None None None None 10.1021/jm980118e
13690207 114870 0 None 29 5 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 114870 0 None 29 5 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
91809277 125220 0 None 1 6 Human 9.5 pKi = 9.5 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 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 125220 0 None 1 6 Human 9.5 pKi = 9.5 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 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
CHEMBL442494 212155 0 None 1 5 Human 9.5 pKi = 9.5 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
13690207 114870 0 None 29 5 Human 9.5 pKi = 9.5 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
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/jm021093t
CHEMBL3350037 114870 0 None 29 5 Human 9.5 pKi = 9.5 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
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/jm021093t
91809303 125244 0 None 1 6 Human 9.5 pKi = 9.5 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 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 125244 0 None 1 6 Human 9.5 pKi = 9.5 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 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
91809276 125219 0 None 4 6 Human 9.5 pKi = 9.5 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 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 125219 0 None 4 6 Human 9.5 pKi = 9.5 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 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
91809278 125221 0 None 48 2 Human 9.5 pKi = 9.5 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 1475 23 16 14 4.0 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)c(F)c2)NC1=O nan
CHEMBL3647679 125221 0 None 48 2 Human 9.5 pKi = 9.5 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 1475 23 16 14 4.0 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)c(F)c2)NC1=O nan
91809298 125239 0 None 575 2 Human 9.5 pKi = 9.5 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 1496 24 16 14 3.4 CC(=O)N(CCCNC[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1)[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 nan
CHEMBL3647697 125239 0 None 575 2 Human 9.5 pKi = 9.5 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 1496 24 16 14 3.4 CC(=O)N(CCCNC[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1)[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 nan
91809317 125841 0 None 22 2 Human 9.4 pKi = 9.4 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 1602 27 18 16 4.2 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](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
CHEMBL3650453 125841 0 None 22 2 Human 9.4 pKi = 9.4 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 1602 27 18 16 4.2 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](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
2055 2851 43 None -1 14 Human 9.4 pKi = 9.4 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 receptor
ChEMBL None None None None 10.1039/C8MD00388B
383414 2851 43 None -1 14 Human 9.4 pKi = 9.4 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 receptor
ChEMBL None None None None 10.1039/C8MD00388B
90488715 2851 43 None -1 14 Human 9.4 pKi = 9.4 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 receptor
ChEMBL None None None None 10.1039/C8MD00388B
CHEMBL1680 2851 43 None -1 14 Human 9.4 pKi = 9.4 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 receptor
ChEMBL None None None None 10.1039/C8MD00388B
CHEMBL262746 2851 43 None -1 14 Human 9.4 pKi = 9.4 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 receptor
ChEMBL None None None None 10.1039/C8MD00388B
DB00104 2851 43 None -1 14 Human 9.4 pKi = 9.4 Binding
Binding affinity to human SST2 receptorBinding affinity to human SST2 receptor
ChEMBL None None None None 10.1039/C8MD00388B
91809308 125249 0 None 4 4 Human 9.4 pKi = 9.4 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 1602 27 18 16 4.2 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](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
CHEMBL3647707 125249 0 None 4 4 Human 9.4 pKi = 9.4 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 1602 27 18 16 4.2 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](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
CHEMBL3098601 209262 0 None -2 5 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-somatostatin from human SSTR2 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR2 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
9851998 24366 0 None 831 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to Somatostatin receptor type 2 was determinedBinding affinity to Somatostatin receptor type 2 was determined
ChEMBL 617 12 4 6 4.3 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCN(C(=O)c2ccccc2)CC1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL134280 24366 0 None 831 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to Somatostatin receptor type 2 was determinedBinding affinity to Somatostatin receptor type 2 was determined
ChEMBL 617 12 4 6 4.3 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCN(C(=O)c2ccccc2)CC1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
2048 2177 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 receptor expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm980194h
70692642 2177 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 receptor expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm980194h
CHEMBL2052017 2177 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 receptor expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm980194h
13690207 114870 0 None 29 5 Human 9.3 pKi = 9.3 Binding
Binding affinity for SSTR2 receptors of rat cortex membranes was determined by using [125I][Tyr3]-octreotide radioligandBinding affinity for SSTR2 receptors of rat cortex membranes was determined by using [125I][Tyr3]-octreotide 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 10.1016/s0960-894x(98)00187-5
CHEMBL3350037 114870 0 None 29 5 Human 9.3 pKi = 9.3 Binding
Binding affinity for SSTR2 receptors of rat cortex membranes was determined by using [125I][Tyr3]-octreotide radioligandBinding affinity for SSTR2 receptors of rat cortex membranes was determined by using [125I][Tyr3]-octreotide 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 10.1016/s0960-894x(98)00187-5
CHEMBL1201185 206849 17 None 7 4 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
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/jm021093t
CHEMBL3349513 209658 0 None 1 4 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) 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](C)NC1=O 10.1021/jm021093t
CHEMBL3349606 209679 0 None -5 4 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None CN(C)CCNC(=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
91809309 125250 0 None 52 2 Human 9.3 pKi = 9.3 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 1602 27 18 16 4.2 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](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
CHEMBL3647708 125250 0 None 52 2 Human 9.3 pKi = 9.3 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 1602 27 18 16 4.2 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](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
91809288 125230 0 None 4 6 Human 9.3 pKi = 9.3 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 125230 0 None 4 6 Human 9.3 pKi = 9.3 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
91809281 125224 0 None 58 2 Human 9.3 pKi = 9.3 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](Cc2ccccc2F)NC1=O nan
CHEMBL3647682 125224 0 None 58 2 Human 9.3 pKi = 9.3 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](Cc2ccccc2F)NC1=O nan
13690207 114870 0 None 29 5 Human 9.2 pKi = 9.2 Binding
Binding affinity towards somatostatin receptor type 2Binding affinity towards somatostatin receptor type 2
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/jm050376t
CHEMBL3350037 114870 0 None 29 5 Human 9.2 pKi = 9.2 Binding
Binding affinity towards somatostatin receptor type 2Binding affinity towards somatostatin receptor type 2
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/jm050376t
91809320 125844 0 None 50 3 Human 9.2 pKi = 9.2 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 1897 34 19 18 6.5 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](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(F)cc2)NC1=O nan
CHEMBL3650456 125844 0 None 50 3 Human 9.2 pKi = 9.2 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 1897 34 19 18 6.5 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](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(F)cc2)NC1=O nan
52936722 60894 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 486 6 2 5 6.7 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(N)nc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766091 60894 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 486 6 2 5 6.7 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4ccc(N)nc4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL421362 211516 0 None 14 5 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined 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/jm021093t
13690207 114870 0 None 29 5 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-somatostatin from human sst2a receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst2a 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 114870 0 None 29 5 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-somatostatin from human sst2a receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst2a 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
52936723 60895 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 501 7 1 5 7.2 COc1ccc(-c2cc3c(OCC[C@H]4CCCCN4)c(-c4cc(C)cc(C)c4)cnc3cc2Cl)cn1 10.1021/jm101501b
CHEMBL1766092 60895 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 501 7 1 5 7.2 COc1ccc(-c2cc3c(OCC[C@H]4CCCCN4)c(-c4cc(C)cc(C)c4)cnc3cc2Cl)cn1 10.1021/jm101501b
155541853 172464 0 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST2A receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST2A 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 172464 0 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST2A receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST2A 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
91809318 125842 0 None 416 2 Human 9.2 pKi = 9.2 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 1695 29 18 17 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](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CCN(C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)S(C)(=O)=O)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL3650454 125842 0 None 416 2 Human 9.2 pKi = 9.2 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 1695 29 18 17 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](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CCN(C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)S(C)(=O)=O)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
91809274 125217 0 None 63 2 Human 9.1 pKi = 9.1 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 1453 24 16 13 4.7 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](CCCNC(=N)N)NC(=O)[C@H](NCCCCC[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
CHEMBL3647675 125217 0 None 63 2 Human 9.1 pKi = 9.1 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 1453 24 16 13 4.7 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](CCCNC(=N)N)NC(=O)[C@H](NCCCCC[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
91809304 125245 0 None 52 2 Human 9.1 pKi = 9.1 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 1538 24 15 14 3.6 CC(=O)N(CCCN(C(C)=O)[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)C[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 nan
CHEMBL3647703 125245 0 None 52 2 Human 9.1 pKi = 9.1 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 1538 24 15 14 3.6 CC(=O)N(CCCN(C(C)=O)[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)C[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 nan
91809314 125255 0 None 234 2 Human 9.1 pKi = 9.1 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 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](Cc2cccnc2)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
CHEMBL3647713 125255 0 None 234 2 Human 9.1 pKi = 9.1 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 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](Cc2cccnc2)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
155547005 173070 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 2030 37 15 32 6.3 CO[C@H]1C[C@H]2OC[C@@]2(OC(C)=O)[C@H]2[C@H](OC(=O)c3ccccc3)[C@]3(O)C[C@H](OC(=O)[C@H](OC(=O)OCCSSCCCN[C@H](Cc4ccccc4)C(=O)N[C@H]4CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc5c[nH]c6ccccc56)NC(=O)[C@H](Cc5ccccc5)NC4=O)[C@@H](NC(=O)OC(C)(C)C)c4ccccc4)C(C)=C([C@@H](OC)C(=O)[C@]12C)C3(C)C 10.1021/acs.jmedchem.8b02036
CHEMBL4534477 173070 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 2030 37 15 32 6.3 CO[C@H]1C[C@H]2OC[C@@]2(OC(C)=O)[C@H]2[C@H](OC(=O)c3ccccc3)[C@]3(O)C[C@H](OC(=O)[C@H](OC(=O)OCCSSCCCN[C@H](Cc4ccccc4)C(=O)N[C@H]4CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc5c[nH]c6ccccc56)NC(=O)[C@H](Cc5ccccc5)NC4=O)[C@@H](NC(=O)OC(C)(C)C)c4ccccc4)C(C)=C([C@@H](OC)C(=O)[C@]12C)C3(C)C 10.1021/acs.jmedchem.8b02036
91809273 125216 0 None 8 2 Human 9.1 pKi = 9.1 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 1439 23 16 13 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](NCCCC[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
CHEMBL3647674 125216 0 None 8 2 Human 9.1 pKi = 9.1 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 1439 23 16 13 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](NCCCC[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
CHEMBL3349599 209672 0 None -2 5 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) 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
CHEMBL3349601 209674 0 None 1 4 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) 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](Cc2c[nH]cn2)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
CHEMBL3349605 209678 0 None -3 4 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) 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](Cc2ccc(O)cc2)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
155563809 174817 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1987 33 15 32 5.1 CO[C@H]1C[C@H]2OC[C@@]2(OC(C)=O)[C@H]2[C@H](OC(=O)c3ccccc3)[C@]3(O)C[C@H](OC(=O)[C@H](OC(=O)OCCSSC[C@H](NC(=O)[C@@H]4CSSC[C@H](NC(=O)[C@H](N)Cc5ccccc5)C(=O)N[C@@H](Cc5ccc(O)cc5)C(=O)N[C@H](Cc5c[nH]c6ccccc56)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N4)C(N)=O)[C@@H](NC(=O)OC(C)(C)C)c4ccccc4)C(C)=C([C@@H](OC)C(=O)[C@]12C)C3(C)C 10.1021/acs.jmedchem.8b02036
CHEMBL4575530 174817 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1987 33 15 32 5.1 CO[C@H]1C[C@H]2OC[C@@]2(OC(C)=O)[C@H]2[C@H](OC(=O)c3ccccc3)[C@]3(O)C[C@H](OC(=O)[C@H](OC(=O)OCCSSC[C@H](NC(=O)[C@@H]4CSSC[C@H](NC(=O)[C@H](N)Cc5ccccc5)C(=O)N[C@@H](Cc5ccc(O)cc5)C(=O)N[C@H](Cc5c[nH]c6ccccc56)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N4)C(N)=O)[C@@H](NC(=O)OC(C)(C)C)c4ccccc4)C(C)=C([C@@H](OC)C(=O)[C@]12C)C3(C)C 10.1021/acs.jmedchem.8b02036
2018 2946 22 None -7 4 Human 9.0 pKi = 9 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
9941444 2946 22 None -7 4 Human 9.0 pKi = 9 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL3349607 2946 22 None -7 4 Human 9.0 pKi = 9 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
DB06663 2946 22 None -7 4 Human 9.0 pKi = 9 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL3349524 209667 0 None -1 4 Human 9.0 pKi = 9 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) 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(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)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
44364081 120363 0 None - 1 Human 9.0 pKi = 9 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 563 14 5 5 4.5 C[C@@H](c1c[nH]c2ccccc12)[C@@H](NC(=O)NCCCc1ccccc1)C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(99)00016-5
CHEMBL355923 120363 0 None - 1 Human 9.0 pKi = 9 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 563 14 5 5 4.5 C[C@@H](c1c[nH]c2ccccc12)[C@@H](NC(=O)NCCCc1ccccc1)C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(99)00016-5
CHEMBL1791304 207168 0 None 25 2 Human 9.0 pKi = 9 Binding
Inhibition of human somatostatin receptor type 2Inhibition of human somatostatin receptor type 2
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
CHEMBL1791312 207172 0 None 123 2 Human 9.0 pKi = 9 Binding
Inhibition of human somatostatin receptor type 2Inhibition of human somatostatin receptor type 2
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
91809309 125250 0 None 52 2 Human 9.0 pKi = 9.0 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 1602 27 18 16 4.2 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](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
CHEMBL3647708 125250 0 None 52 2 Human 9.0 pKi = 9.0 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 1602 27 18 16 4.2 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](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
44364008 40264 0 None - 1 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 595 11 3 5 4.4 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)NC[C@H]1OC[C@H](N)CO1)N1CCN(CCC(c2ccccc2)c2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL148309 40264 0 None - 1 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 595 11 3 5 4.4 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)NC[C@H]1OC[C@H](N)CO1)N1CCN(CCC(c2ccccc2)c2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL410194 211050 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for SSTR2 receptors of rat cortex membranes was determined by using [125I][Tyr3]-octreotide radioligandBinding affinity for SSTR2 receptors of rat cortex membranes was determined by using [125I][Tyr3]-octreotide radioligand
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](CCCCNC(=O)OC(C)(C)C)C(=O)N[C@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1016/s0960-894x(98)00187-5
CHEMBL3349517 209662 0 None -3 4 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) 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(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](C)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
44363919 118650 0 None - 1 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 629 12 3 5 5.6 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(Cc2ccc(C(F)(F)F)cc2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL343010 118650 0 None - 1 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 629 12 3 5 5.6 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(Cc2ccc(C(F)(F)F)cc2)C1=O 10.1016/s0960-894x(99)00016-5
91809319 125843 0 None 1 3 Human 8.9 pKi = 8.9 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 1453 22 16 14 3.3 C[C@@H](O)C1NC(=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(=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
CHEMBL3650455 125843 0 None 1 3 Human 8.9 pKi = 8.9 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 1453 22 16 14 3.3 C[C@@H](O)C1NC(=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(=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
91809313 125254 0 None 1 3 Human 8.9 pKi = 8.9 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 1616 26 18 16 3.7 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](CCCNC(=N)N)NC(=O)[C@H](NC(=O)[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
CHEMBL3647712 125254 0 None 1 3 Human 8.9 pKi = 8.9 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 1616 26 18 16 3.7 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](CCCNC(=N)N)NC(=O)[C@H](NC(=O)[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
44364016 118776 0 None - 1 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 630 12 3 6 5.0 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(C2CCCN(c3ccccc3)C2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL343897 118776 0 None - 1 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 630 12 3 6 5.0 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(C2CCCN(c3ccccc3)C2)C1=O 10.1016/s0960-894x(99)00016-5
24951595 60904 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 474 6 1 5 6.5 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cnn(C)c4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766101 60904 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 474 6 1 5 6.5 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cnn(C)c4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1021/jm101501b
54580404 60910 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 504 6 2 3 7.2 Cc1cc(C)cc(-c2c(OCC[C@H]3CCCCN3)c3cc(-c4ccc(F)cc4)c(Cl)cc3[nH]c2=O)c1 10.1021/jm101501b
CHEMBL1766107 60910 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 504 6 2 3 7.2 Cc1cc(C)cc(-c2c(OCC[C@H]3CCCCN3)c3cc(-c4ccc(F)cc4)c(Cl)cc3[nH]c2=O)c1 10.1021/jm101501b
CHEMBL262017 208771 0 None 7 2 Human 8.8 pKi = 8.8 Binding
Binding affinity towards somatostatin receptor type 2Binding affinity towards somatostatin receptor type 2
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=O)[C@@H](C)O)NC1=O 10.1021/jm050376t
44397706 66840 0 None 1 5 Human 8.7 pKi = 8.7 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 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 66840 0 None 1 5 Human 8.7 pKi = 8.7 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 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
CHEMBL3349602 209675 0 None -5 5 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) 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
44355051 96104 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 617 12 4 6 4.3 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)c2ccccc2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL263024 96104 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 617 12 4 6 4.3 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)c2ccccc2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
44354261 116291 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 675 13 4 8 3.9 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)Cc2ccc3c(c2)OCO3)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL337846 116291 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 675 13 4 8 3.9 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)Cc2ccc3c(c2)OCO3)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
44354528 170783 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 633 14 4 7 4.6 COc1cccc(CN2CCCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c3c[nH]c4ccccc34)C2)c1 10.1016/s0960-894x(00)00687-9
CHEMBL446165 170783 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 633 14 4 7 4.6 COc1cccc(CN2CCCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c3c[nH]c4ccccc34)C2)c1 10.1016/s0960-894x(00)00687-9
CHEMBL3349604 209677 0 None -25 5 Human 8.0 pKi = 8 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) 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
44363920 37760 0 None - 1 Mouse 8.0 pKi = 8 Binding
In vitro binding affinity was evaluated against mouse Somatostatin receptor type 2 (mSSTR-2)In vitro binding affinity was evaluated against mouse Somatostatin receptor type 2 (mSSTR-2)
ChEMBL 560 10 3 6 4.0 COC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)OC(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/s0960-894x(99)00016-5
CHEMBL146022 37760 0 None - 1 Mouse 8.0 pKi = 8 Binding
In vitro binding affinity was evaluated against mouse Somatostatin receptor type 2 (mSSTR-2)In vitro binding affinity was evaluated against mouse Somatostatin receptor type 2 (mSSTR-2)
ChEMBL 560 10 3 6 4.0 COC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)OC(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/s0960-894x(99)00016-5
15485372 37890 0 None - 1 Mouse 8.0 pKi = 8 Binding
In vitro binding affinity was evaluated against mouse Somatostatin receptor type 2 (mSSTR-2)In vitro binding affinity was evaluated against mouse Somatostatin receptor type 2 (mSSTR-2)
ChEMBL 501 9 4 3 4.0 NCCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/s0960-894x(99)00016-5
CHEMBL146128 37890 0 None - 1 Mouse 8.0 pKi = 8 Binding
In vitro binding affinity was evaluated against mouse Somatostatin receptor type 2 (mSSTR-2)In vitro binding affinity was evaluated against mouse Somatostatin receptor type 2 (mSSTR-2)
ChEMBL 501 9 4 3 4.0 NCCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/s0960-894x(99)00016-5
44397628 67036 0 None -3 2 Human 7.0 pKi = 7 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 441 9 2 5 5.7 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.061
CHEMBL188767 67036 0 None -3 2 Human 7.0 pKi = 7 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 441 9 2 5 5.7 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.061
CHEMBL2369753 207916 0 None -11 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
CHEMBL2369759 207922 0 None -1 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
CHEMBL3349515 209660 0 None -12 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) 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(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](C)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
CHEMBL3349525 209668 0 None -10 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) 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(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](C)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
9959684 33710 0 None -2 2 Human 6.0 pKi = 6 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 33710 0 None -2 2 Human 6.0 pKi = 6 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
10601454 35068 0 None 1 2 Human 6.0 pKi = 6 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 35068 0 None 1 2 Human 6.0 pKi = 6 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
10838621 202389 0 None - 1 Human 5.0 pKi = 5 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 receptor expressed in CHO-K1 cells
ChEMBL 485 8 4 3 3.7 NCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/jm980194h
CHEMBL70224 202389 0 None - 1 Human 5.0 pKi = 5 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 receptor expressed in CHO-K1 cells
ChEMBL 485 8 4 3 3.7 NCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/jm980194h
CHEMBL411556 211129 0 None -1 4 Human 7.0 pKi = 7.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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(F)c2)CSSC[C@@H](C(=O)N[C@@H](Cc2cccc(F)c2)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL412561 211247 0 None 6 3 Human 7.0 pKi = 7.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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(F)cc2)CSSC[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(N)=O)NC1=O 10.1021/jm9806289
44355050 96103 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 661 14 4 8 4.4 COC(=O)c1cccc(CN2CCCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c3c[nH]c4ccccc34)C2)c1 10.1016/s0960-894x(00)00687-9
CHEMBL263023 96103 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 661 14 4 8 4.4 COC(=O)c1cccc(CN2CCCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c3c[nH]c4ccccc34)C2)c1 10.1016/s0960-894x(00)00687-9
44354613 114605 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 632 12 5 6 4.7 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)Nc2ccccc2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL334340 114605 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 632 12 5 6 4.7 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)Nc2ccccc2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
44354650 116031 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 671 13 4 7 4.0 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(S(=O)(=O)c2ccc(F)cc2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL336286 116031 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 671 13 4 7 4.0 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(S(=O)(=O)c2ccc(F)cc2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
44364114 120512 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 533 10 2 5 3.2 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N(C)C[C@H]1OC[C@H](N)CO1)N1CCN(CCCc2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL356717 120512 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 533 10 2 5 3.2 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N(C)C[C@H]1OC[C@H](N)CO1)N1CCN(CCCc2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL2371893 208392 0 None 3 5 Human 8.0 pKi = 8.0 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
168275406 189703 0 None -1000 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 189703 0 None -1000 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
44308810 202365 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 receptor expressed in CHO-K1 cells
ChEMBL 543 10 5 4 3.5 NCCCCC(NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1)C(=O)O 10.1021/jm980194h
CHEMBL70096 202365 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 receptor expressed in CHO-K1 cells
ChEMBL 543 10 5 4 3.5 NCCCCC(NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1)C(=O)O 10.1021/jm980194h
CHEMBL2369761 207924 0 None 5 5 Human 6.9 pKi = 6.9 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
CHEMBL406152 210839 0 None -1 4 Human 6.9 pKi = 6.9 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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(F)c2)CSSC[C@H](C(=O)N[C@@H](Cc2cccc(F)c2)C(N)=O)NC1=O 10.1021/jm9806289
44354529 25116 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 681 13 4 8 5.0 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(Cc2ccc3c(c2Cl)OCO3)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL134923 25116 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 681 13 4 8 5.0 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(Cc2ccc3c(c2Cl)OCO3)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
44364017 118699 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 603 14 3 5 5.4 CC(CCc1ccccc1)N1CCN([C@@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c2c[nH]c3ccccc23)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL343347 118699 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 603 14 3 5 5.4 CC(CCc1ccccc1)N1CCN([C@@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c2c[nH]c3ccccc23)C1=O 10.1016/s0960-894x(99)00016-5
44397620 67517 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 442 9 2 6 5.0 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL191025 67517 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 442 9 2 6 5.0 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
44397472 124521 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 460 9 2 6 5.2 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2cc(F)ccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL364418 124521 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 460 9 2 6 5.2 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2cc(F)ccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL2372961 208572 0 None 8 4 Human 7.9 pKi = 7.9 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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
CHEMBL408347 210950 0 None 3 4 Human 7.9 pKi = 7.9 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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/jm9806289
CHEMBL2369749 207912 0 None 3 5 Human 7.9 pKi = 7.9 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
44354386 22394 0 None 30 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to Somatostatin receptor type 2 was determinedBinding affinity to Somatostatin receptor type 2 was determined
ChEMBL 619 13 4 7 3.2 CC(C)S(=O)(=O)N1CCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00687-9
CHEMBL132658 22394 0 None 30 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to Somatostatin receptor type 2 was determinedBinding affinity to Somatostatin receptor type 2 was determined
ChEMBL 619 13 4 7 3.2 CC(C)S(=O)(=O)N1CCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00687-9
10720221 34848 0 None -1 2 Human 4.9 pKi = 4.9 Binding
In vitro binding affinity at sst2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at sst2 receptor in transfected HEK 293 cell 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 34848 0 None -1 2 Human 4.9 pKi = 4.9 Binding
In vitro binding affinity at sst2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at sst2 receptor in transfected HEK 293 cell 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
44364006 118064 0 None - 1 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 555 9 3 5 3.6 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)NC[C@H]1OC[C@H](N)CO1)N1CCN(CCc2cccc3ccccc23)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL341645 118064 0 None - 1 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 555 9 3 5 3.6 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)NC[C@H]1OC[C@H](N)CO1)N1CCN(CCc2cccc3ccccc23)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL2372964 208575 0 None 1 4 Human 6.9 pKi = 6.9 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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
44354615 24149 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 659 13 4 8 3.9 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(S(=O)(=O)c2cccs2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL134111 24149 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 659 13 4 8 3.9 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(S(=O)(=O)c2cccs2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
44363998 40205 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 561 12 3 5 4.5 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(Cc2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL148255 40205 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 561 12 3 5 4.5 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(Cc2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
10053855 167978 0 None 263 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 in experiment 2In vitro binding affinity was evaluated against human Somatostatin receptor type 2 in experiment 2
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 167978 0 None 263 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 in experiment 2In vitro binding affinity was evaluated against human Somatostatin receptor type 2 in experiment 2
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
CHEMBL385746 210607 0 None 3 4 Human 7.9 pKi = 7.9 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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](Cc2ccccn2)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
54582417 60909 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 488 6 2 5 5.8 Cc1cc(C)cc(-c2c(OCCC3CCCCN3)c3cc(-c4ccncn4)c(Cl)cc3[nH]c2=O)c1 10.1021/jm101501b
CHEMBL1766106 60909 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 488 6 2 5 5.8 Cc1cc(C)cc(-c2c(OCCC3CCCCN3)c3cc(-c4ccncn4)c(Cl)cc3[nH]c2=O)c1 10.1021/jm101501b
44354398 114990 0 None 190 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to Somatostatin receptor type 2 was determinedBinding affinity to Somatostatin receptor type 2 was determined
ChEMBL 583 12 4 6 3.6 CC(C)C(=O)N1CCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00687-9
CHEMBL335223 114990 0 None 190 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to Somatostatin receptor type 2 was determinedBinding affinity to Somatostatin receptor type 2 was determined
ChEMBL 583 12 4 6 3.6 CC(C)C(=O)N1CCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00687-9
44397990 67657 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 441 9 2 5 5.7 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cccc2ccccc12 10.1016/j.bmcl.2005.05.061
CHEMBL191255 67657 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 441 9 2 5 5.7 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cccc2ccccc12 10.1016/j.bmcl.2005.05.061
CHEMBL408787 210975 0 None 28 3 Human 7.8 pKi = 7.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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)C(c2ccccc2)c2ccccc2)CSSC[C@@H](C(=O)N[C@H](C(N)=O)C(c2ccccc2)c2ccccc2)NC1=O 10.1021/jm9806289
CHEMBL437448 211961 0 None 3 5 Human 7.8 pKi = 7.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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
44397907 67607 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 447 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cc2ccccc2s1 10.1016/j.bmcl.2005.05.061
CHEMBL191171 67607 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 447 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cc2ccccc2s1 10.1016/j.bmcl.2005.05.061
10769191 33555 0 None -3 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 33555 0 None -3 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
CHEMBL408987 210983 0 None 1 5 Human 6.8 pKi = 6.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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
CHEMBL429166 211751 0 None -1 4 Human 6.8 pKi = 6.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
ChEMBL None None None CC(C)(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)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
142471801 191691 0 None -933 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 191691 0 None -933 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
44354527 25319 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 653 13 4 6 5.8 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(Cc2ccc3ccccc3c2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL135099 25319 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 653 13 4 6 5.8 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(Cc2ccc3ccccc3c2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL2369755 207918 0 None -2 5 Human 7.8 pKi = 7.8 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
10841338 33870 0 None -3 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 33870 0 None -3 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
10578474 33950 0 None -3 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 33950 0 None -3 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
168272497 189629 0 None -3467 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 189629 0 None -3467 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
44308969 202651 0 None -1096 5 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 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 202651 0 None -1096 5 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 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
CHEMBL406491 210854 0 None -4 4 Human 6.8 pKi = 6.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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)Cc2ccccc2F)CSSC[C@@H](C(=O)N[C@@H](Cc2ccccc2F)C(N)=O)NC1=O 10.1021/jm9806289
44354651 168028 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 513 11 5 6 2.7 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCNC1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL435981 168028 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 513 11 5 6 2.7 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCNC1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
44363956 39831 0 None - 1 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 519 10 3 5 2.8 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)NC[C@H]1OC[C@H](N)CO1)N1CCN(CCCc2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL147939 39831 0 None - 1 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 519 10 3 5 2.8 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)NC[C@H]1OC[C@H](N)CO1)N1CCN(CCCc2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
9852911 98911 0 None -19 6 Human 5.8 pKi = 5.8 Binding
Binding affinity for human receptor subtype hSSTR2Binding affinity for human receptor subtype hSSTR2
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 98911 0 None -19 6 Human 5.8 pKi = 5.8 Binding
Binding affinity for human receptor subtype hSSTR2Binding affinity for human receptor subtype hSSTR2
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
CHEMBL2369756 207919 0 None 2 5 Human 6.7 pKi = 6.7 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
CHEMBL2372957 208568 0 None 3 4 Human 7.7 pKi = 7.7 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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
CHEMBL3349514 209659 0 None 5 4 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) 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(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/jm021093t
CHEMBL3349520 209664 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) 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(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](C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm021093t
CHEMBL413709 211325 0 None 2 3 Human 6.7 pKi = 6.7 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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)c(I)c2)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
CHEMBL2369733 207906 0 None 5 5 Human 6.7 pKi = 6.7 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
44363921 39297 0 None - 1 Mouse 8.7 pKi = 8.7 Binding
In vitro binding affinity was evaluated against mouse Somatostatin receptor type 2 (mSSTR-2)In vitro binding affinity was evaluated against mouse Somatostatin receptor type 2 (mSSTR-2)
ChEMBL 559 10 4 5 3.6 COC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/s0960-894x(99)00016-5
CHEMBL147319 39297 0 None - 1 Mouse 8.7 pKi = 8.7 Binding
In vitro binding affinity was evaluated against mouse Somatostatin receptor type 2 (mSSTR-2)In vitro binding affinity was evaluated against mouse Somatostatin receptor type 2 (mSSTR-2)
ChEMBL 559 10 4 5 3.6 COC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/s0960-894x(99)00016-5
11705763 167741 0 None -5 5 Human 8.7 pKi = 8.7 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 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 167741 0 None -5 5 Human 8.7 pKi = 8.7 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 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
13690207 114870 0 None 29 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human SSTR2ABinding affinity to human SSTR2A
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 10.1016/j.bmcl.2008.07.027
CHEMBL3350037 114870 0 None 29 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human SSTR2ABinding affinity to human SSTR2A
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 10.1016/j.bmcl.2008.07.027
10053855 167978 0 None 263 2 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 in experiment 1In vitro binding affinity was evaluated against human Somatostatin receptor type 2 in experiment 1
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 167978 0 None 263 2 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 in experiment 1In vitro binding affinity was evaluated against human Somatostatin receptor type 2 in experiment 1
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
44364080 39578 0 None - 1 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 577 14 4 5 4.9 C[C@@H](c1c[nH]c2ccccc12)[C@@H](NC(=O)N(C)CCCc1ccccc1)C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(99)00016-5
CHEMBL147711 39578 0 None - 1 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 577 14 4 5 4.9 C[C@@H](c1c[nH]c2ccccc12)[C@@H](NC(=O)N(C)CCCc1ccccc1)C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(99)00016-5
91809302 125243 0 None 26 3 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 1439 23 16 14 3.7 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](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](Cc2ccccc2)NC1=O nan
CHEMBL3647701 125243 0 None 26 3 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 1439 23 16 14 3.7 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](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](Cc2ccccc2)NC1=O nan
44354297 116133 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 667 13 4 6 4.5 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)Cc2cc(F)cc(F)c2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL336986 116133 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 667 13 4 6 4.5 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)Cc2cc(F)cc(F)c2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL2370167 208051 0 None 45 5 Human 8.6 pKi = 8.6 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst2) expressed in CHO-K1 cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst2) expressed in CHO-K1 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
44354415 116107 0 None 131 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to Somatostatin receptor type 2 was determinedBinding affinity to Somatostatin receptor type 2 was determined
ChEMBL 603 13 4 6 4.6 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCN(Cc2ccccc2)CC1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL336819 116107 0 None 131 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to Somatostatin receptor type 2 was determinedBinding affinity to Somatostatin receptor type 2 was determined
ChEMBL 603 13 4 6 4.6 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCN(Cc2ccccc2)CC1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
44397389 123513 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 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 123513 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 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
44354586 24216 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 723 14 5 7 4.9 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)C(O)(c2ccccc2)c2ccccc2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL134163 24216 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 723 14 5 7 4.9 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)C(O)(c2ccccc2)c2ccccc2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
44354505 114918 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 639 13 4 6 4.9 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(Cc2ccc(F)c(F)c2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL335045 114918 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 639 13 4 6 4.9 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(Cc2ccc(F)c(F)c2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
44309052 202240 0 None 109 5 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 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 202240 0 None 109 5 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 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
54584354 60911 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 515 7 2 6 6.1 Cc1cc(C)cc(-c2cnc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766108 60911 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation countingDisplacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting
ChEMBL 515 7 2 6 6.1 Cc1cc(C)cc(-c2cnc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL2369719 207902 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Inhibition of human somatostatin receptor type 2Inhibition of human somatostatin receptor type 2
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
CHEMBL2369720 207903 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of human somatostatin receptor type 2Inhibition of human somatostatin receptor type 2
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](C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm058184l
CHEMBL407195 210889 0 None 6 4 Human 7.7 pKi = 7.7 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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(F)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(N)=O)NC1=O 10.1021/jm9806289
10768264 34614 0 None -2 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 34614 0 None -2 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
11800917 34872 0 None -20 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 34872 0 None -20 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
10745635 118829 0 None -1 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 118829 0 None -1 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
CHEMBL414116 211353 0 None 1 4 Human 6.7 pKi = 6.7 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
ChEMBL None None None 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
142471848 190663 0 None -2089 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 190663 0 None -2089 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
44354584 114696 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 679 14 4 6 6.3 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(Cc2ccccc2-c2ccccc2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL334499 114696 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 679 14 4 6 6.3 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(Cc2ccccc2-c2ccccc2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
44377555 57212 0 None -3 5 Human 5.7 pKi = 5.7 Binding
Inhibitory constant on human Somatostatin receptor type 2Inhibitory constant on human Somatostatin receptor type 2
ChEMBL 384 5 1 5 5.2 NCCCc1nc(-c2csc3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
CHEMBL166247 57212 0 None -3 5 Human 5.7 pKi = 5.7 Binding
Inhibitory constant on human Somatostatin receptor type 2Inhibitory constant on human Somatostatin receptor type 2
ChEMBL 384 5 1 5 5.2 NCCCc1nc(-c2csc3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
44397788 67038 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 430 9 3 5 5.0 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cccc2cc[nH]c12 10.1016/j.bmcl.2005.05.061
CHEMBL188777 67038 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 430 9 3 5 5.0 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cccc2cc[nH]c12 10.1016/j.bmcl.2005.05.061
10650427 34197 0 None -1 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 34197 0 None -1 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
CHEMBL264539 208873 0 None -3 3 Human 5.7 pKi = 5.7 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(-c3ccccc3)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(N)=O)NC1=O 10.1021/jm9806289
44308782 102776 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 receptor expressed in CHO-K1 cells
ChEMBL 513 10 4 3 4.5 NCCCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/jm980194h
CHEMBL308444 102776 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 receptor expressed in CHO-K1 cells
ChEMBL 513 10 4 3 4.5 NCCCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/jm980194h
44354689 115954 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 597 13 4 6 4.0 CC(C)CC(=O)N1CCCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c2c[nH]c3ccccc23)C1 10.1016/s0960-894x(00)00687-9
CHEMBL336108 115954 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 597 13 4 6 4.0 CC(C)CC(=O)N1CCCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c2c[nH]c3ccccc23)C1 10.1016/s0960-894x(00)00687-9
44354649 167867 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 713 15 4 9 3.8 COc1ccc(S(=O)(=O)N2CCCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c3c[nH]c4ccccc34)C2)cc1OC 10.1016/s0960-894x(00)00687-9
CHEMBL434991 167867 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 713 15 4 9 3.8 COc1ccc(S(=O)(=O)N2CCCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c3c[nH]c4ccccc34)C2)cc1OC 10.1016/s0960-894x(00)00687-9
44397924 67229 0 None -2 2 Human 7.6 pKi = 7.6 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 512 10 2 7 6.0 Cc1cccc2c(C(=O)C(C)(C)CSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
CHEMBL190070 67229 0 None -2 2 Human 7.6 pKi = 7.6 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 512 10 2 7 6.0 Cc1cccc2c(C(=O)C(C)(C)CSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
10505242 33605 0 None 1 2 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 33605 0 None 1 2 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
CHEMBL385745 210606 0 None -2 4 Human 6.6 pKi = 6.6 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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](Cc2ccccn2)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
CHEMBL2369757 207920 0 None 12 5 Human 7.6 pKi = 7.6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
CHEMBL438281 212005 0 None -1 4 Human 6.6 pKi = 6.6 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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)Cc2ccccc2F)CSSC[C@H](C(=O)N[C@@H](Cc2ccccc2F)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL437220 211953 0 None 3 4 Human 7.6 pKi = 7.6 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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
44397747 66780 0 None -4 2 Human 6.6 pKi = 6.6 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 469 9 2 5 5.3 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cccc(Br)c1 10.1016/j.bmcl.2005.05.061
CHEMBL187498 66780 0 None -4 2 Human 6.6 pKi = 6.6 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 469 9 2 5 5.3 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cccc(Br)c1 10.1016/j.bmcl.2005.05.061
9872511 121492 0 None -21 2 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 121492 0 None -21 2 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
CHEMBL2372959 208570 0 None 1 5 Human 6.6 pKi = 6.6 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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
CHEMBL510755 213802 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned sst2 receptorBinding affinity to human cloned sst2 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)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL2311098 207750 0 None 4 5 Human 7.6 pKi = 7.6 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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/jm9806289
CHEMBL2372963 208574 0 None 8 3 Human 7.6 pKi = 7.6 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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
10770814 100312 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity for human receptor subtype hSSTR2Binding affinity for human receptor subtype hSSTR2
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 100312 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity for human receptor subtype hSSTR2Binding affinity for human receptor subtype hSSTR2
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
9893924 4665 27 None -52 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST2A receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST2A 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 4665 27 None -52 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST2A receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST2A 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
127029955 138344 0 None -2 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]tyr11-SRIF from human sst2 receptor after 60 mins by liquid scintillation counting methodDisplacement of [125I]tyr11-SRIF from human sst2 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 138344 0 None -2 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]tyr11-SRIF from human sst2 receptor after 60 mins by liquid scintillation counting methodDisplacement of [125I]tyr11-SRIF from human sst2 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 138344 0 None -2 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]tyr11-SRIF from human sst2 receptor after 60 mins by liquid scintillation counting methodDisplacement of [125I]tyr11-SRIF from human sst2 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
CHEMBL2369758 207921 0 None 5 5 Human 7.6 pKi = 7.6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
10699714 98945 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity for human receptor subtype hSSTR2Binding affinity for human receptor subtype hSSTR2
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 98945 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity for human receptor subtype hSSTR2Binding affinity for human receptor subtype hSSTR2
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
90665460 108760 0 None -12 5 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-somatostatin from human sst2a receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst2a 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 108760 0 None -12 5 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-somatostatin from human sst2a receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst2a 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
44397815 67400 0 None -2 2 Human 5.6 pKi = 5.6 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 469 10 1 5 6.3 CN(C)CCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.061
CHEMBL190786 67400 0 None -2 2 Human 5.6 pKi = 5.6 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 469 10 1 5 6.3 CN(C)CCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.061
CHEMBL2370166 208050 0 None 7 5 Human 7.5 pKi = 7.5 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst2) expressed in CHO-K1 cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst2) 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
CHEMBL407643 210916 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for SSTR2 receptors of rat cortex membranes was determined by using [125I][Tyr3]-octreotide radioligandBinding affinity for SSTR2 receptors of rat cortex membranes was determined by using [125I][Tyr3]-octreotide radioligand
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](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCNC(=O)OC(C)(C)C)C(=O)N[C@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1016/s0960-894x(98)00187-5
CHEMBL3349603 209676 0 None -5 5 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) 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
91809316 125840 0 None 141 2 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 1737 28 16 16 7.3 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](N(CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3650452 125840 0 None 141 2 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 1737 28 16 16 7.3 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](N(CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
44363816 39422 0 None 22 5 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
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 39422 0 None 22 5 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
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
91809315 125256 0 None 89 2 Human 8.4 pKi = 8.4 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 1755 28 16 16 7.5 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](N(CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCSC[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
CHEMBL3647714 125256 0 None 89 2 Human 8.4 pKi = 8.4 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 1755 28 16 16 7.5 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](N(CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCSC[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
10624774 202286 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 receptor expressed in CHO-K1 cells
ChEMBL 485 8 4 3 3.7 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/jm980194h
CHEMBL69575 202286 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 receptor expressed in CHO-K1 cells
ChEMBL 485 8 4 3 3.7 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/jm980194h
10554709 118796 0 None -3 2 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 118796 0 None -3 2 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
44354552 25318 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 679 14 4 6 6.2 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(c2ccccc2)c2ccccc2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL135096 25318 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 679 14 4 6 6.2 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(c2ccccc2)c2ccccc2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL407496 210908 0 None 5 5 Human 7.5 pKi = 7.5 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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
10554498 31059 0 None -4 2 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 31059 0 None -4 2 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
9985523 98691 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Binding affinity for human receptor subtype hSSTR2Binding affinity for human receptor subtype hSSTR2
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 98691 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Binding affinity for human receptor subtype hSSTR2Binding affinity for human receptor subtype hSSTR2
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
90644981 111308 0 None -81 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]SS14 from human SST2 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST2 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 111308 0 None -81 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]SS14 from human SST2 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST2 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
CHEMBL2369760 207923 0 None -13 5 Human 6.5 pKi = 6.5 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
44397385 66961 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 443 9 2 7 4.4 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cnc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL188402 66961 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 443 9 2 7 4.4 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cnc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL264028 208848 0 None -1 5 Human 7.5 pKi = 7.5 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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
CHEMBL439136 212069 0 None 1 4 Human 7.5 pKi = 7.5 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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
44377591 55329 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Inhibitory constant on human Somatostatin receptor type 2Inhibitory constant on human Somatostatin receptor type 2
ChEMBL 536 9 3 6 5.6 CC(C)(C(=O)NCCc1c[nH]c2ccccc12)c1cn2cc(-c3csc4ccccc34)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
CHEMBL162140 55329 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Inhibitory constant on human Somatostatin receptor type 2Inhibitory constant on human Somatostatin receptor type 2
ChEMBL 536 9 3 6 5.6 CC(C)(C(=O)NCCc1c[nH]c2ccccc12)c1cn2cc(-c3csc4ccccc34)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
142471936 190889 0 None -4677 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 190889 0 None -4677 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
10528970 34194 0 None -4 2 Human 4.5 pKi = 4.5 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 34194 0 None -4 2 Human 4.5 pKi = 4.5 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
155566365 175336 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1927 34 17 27 4.2 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](CCCCNC(=O)NCCCCCCN)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
CHEMBL4587303 175336 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 minsDisplacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins
ChEMBL 1927 34 17 27 4.2 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](CCCCNC(=O)NCCCCCCN)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
44387399 168440 0 None 2 3 Human 6.5 pKi = 6.5 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
ChEMBL 1055 13 11 14 1.3 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](NN2Cc3ccccc3CC2C(=O)O)CSSC[C@@H](C(=O)NN2Cc3ccccc3CC2C(=O)O)NC1=O 10.1021/jm9806289
CHEMBL439350 168440 0 None 2 3 Human 6.5 pKi = 6.5 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
ChEMBL 1055 13 11 14 1.3 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](NN2Cc3ccccc3CC2C(=O)O)CSSC[C@@H](C(=O)NN2Cc3ccccc3CC2C(=O)O)NC1=O 10.1021/jm9806289
10166743 123415 0 None -43 5 Human 5.5 pKi = 5.5 Binding
Inhibition of human sst2 receptor expressed in CHO cellsInhibition of human sst2 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 123415 0 None -43 5 Human 5.5 pKi = 5.5 Binding
Inhibition of human sst2 receptor expressed in CHO cellsInhibition of human sst2 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
44354614 23592 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 619 13 4 7 3.2 CC(C)S(=O)(=O)N1CCCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c2c[nH]c3ccccc23)C1 10.1016/s0960-894x(00)00687-9
CHEMBL133612 23592 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 619 13 4 7 3.2 CC(C)S(=O)(=O)N1CCCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c2c[nH]c3ccccc23)C1 10.1016/s0960-894x(00)00687-9
CHEMBL2372960 208571 0 None 4 4 Human 7.5 pKi = 7.5 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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
CHEMBL415201 211422 0 None 7 4 Human 7.5 pKi = 7.5 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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(F)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL2369750 207913 0 None 1 5 Human 7.4 pKi = 7.4 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
44354852 155228 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 661 12 4 8 4.0 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)c2ccc3c(c2)OCO3)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL405921 155228 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 661 12 4 8 4.0 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)c2ccc3c(c2)OCO3)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
168272821 189990 0 None -4677 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 189990 0 None -4677 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
CHEMBL412859 211274 0 None 19 3 Human 7.4 pKi = 7.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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](C(N)=O)C(c2ccccc2)c2ccccc2)NC1=O 10.1021/jm9806289
142471924 189790 0 None -4466 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 189790 0 None -4466 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
44308836 102305 0 None 134 5 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 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 102305 0 None 134 5 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 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
44397648 66416 0 None 2 5 Human 8.4 pKi = 8.4 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 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 66416 0 None 2 5 Human 8.4 pKi = 8.4 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 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
91809311 125252 0 None 66 2 Human 8.3 pKi = 8.3 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 1471 22 16 14 3.4 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(=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
CHEMBL3647710 125252 0 None 66 2 Human 8.3 pKi = 8.3 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 1471 22 16 14 3.4 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(=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
44354850 116156 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 603 13 4 6 4.6 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(Cc2ccccc2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL337083 116156 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 603 13 4 6 4.6 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(Cc2ccccc2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
44364113 118864 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 609 11 2 5 4.8 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N(C)C[C@H]1OC[C@H](N)CO1)N1CCN(CCC(c2ccccc2)c2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL344511 118864 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 609 11 2 5 4.8 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N(C)C[C@H]1OC[C@H](N)CO1)N1CCN(CCC(c2ccccc2)c2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
44364007 118065 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 575 10 4 8 2.3 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)NC[C@H]1OC[C@H](N)CO1)N1CCN(CCCn2c(O)nc3ccccc32)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL341646 118065 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 575 10 4 8 2.3 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)NC[C@H]1OC[C@H](N)CO1)N1CCN(CCCn2c(O)nc3ccccc32)C1=O 10.1016/s0960-894x(99)00016-5
44363954 38392 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 in experiment 1In vitro binding affinity was evaluated against human Somatostatin receptor type 2 in experiment 1
ChEMBL 629 12 3 5 6.1 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(C2CCC(c3ccccc3)CC2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL146536 38392 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 in experiment 1In vitro binding affinity was evaluated against human Somatostatin receptor type 2 in experiment 1
ChEMBL 629 12 3 5 6.1 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(C2CCC(c3ccccc3)CC2)C1=O 10.1016/s0960-894x(99)00016-5
168288485 191125 0 None -7943 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 191125 0 None -7943 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
CHEMBL2372958 208569 0 None 1 3 Human 6.4 pKi = 6.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CS2=CCc3ccccc32)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
10436888 118793 0 None -295 2 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 118793 0 None -295 2 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
44385504 60708 0 None -10 5 Human 5.4 pKi = 5.4 Binding
Inhibition of human sst2 receptor expressed in CHO cellsInhibition of human sst2 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 60708 0 None -10 5 Human 5.4 pKi = 5.4 Binding
Inhibition of human sst2 receptor expressed in CHO cellsInhibition of human sst2 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
44397875 126527 0 None -16 2 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 419 10 2 5 5.1 CCc1ccc(-c2nnc(SCCc3c[nH]c4ccccc34)n2CCCCN)cc1 10.1016/j.bmcl.2005.05.061
CHEMBL365627 126527 0 None -16 2 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 419 10 2 5 5.1 CCc1ccc(-c2nnc(SCCc3c[nH]c4ccccc34)n2CCCCN)cc1 10.1016/j.bmcl.2005.05.061
90665461 108761 0 None -25 5 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]-somatostatin from human sst2a receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst2a 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 108761 0 None -25 5 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]-somatostatin from human sst2a receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst2a 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
9852911 98911 0 None -19 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to sst2 receptor (unknown origin)Binding affinity to sst2 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 98911 0 None -19 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to sst2 receptor (unknown origin)Binding affinity to sst2 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
9827283 78163 0 None 56 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 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 78163 0 None 56 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 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
10554930 99716 0 None -1 5 Human 5.3 pKi = 5.3 Binding
Binding affinity for human receptor subtype hSSTR2Binding affinity for human receptor subtype hSSTR2
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 99716 0 None -1 5 Human 5.3 pKi = 5.3 Binding
Binding affinity for human receptor subtype hSSTR2Binding affinity for human receptor subtype hSSTR2
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
10325243 100016 0 None -2 5 Human 5.3 pKi = 5.3 Binding
Binding affinity for human receptor subtype hSSTR2Binding affinity for human receptor subtype hSSTR2
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 100016 0 None -2 5 Human 5.3 pKi = 5.3 Binding
Binding affinity for human receptor subtype hSSTR2Binding affinity for human receptor subtype hSSTR2
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
100930865 34552 0 None -91 2 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 34552 0 None -91 2 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 34552 0 None -91 2 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
127032867 138328 0 None -2 2 Human 5.3 pKi = 5.3 Binding
Binding affinity to human sst2 receptorBinding affinity to human sst2 receptor
ChEMBL 338 10 2 3 4.3 NCCCCCOc1ccccc1OCCc1c[nH]c2ccccc12 10.1016/j.ejmech.2016.02.046
CHEMBL3781875 138328 0 None -2 2 Human 5.3 pKi = 5.3 Binding
Binding affinity to human sst2 receptorBinding affinity to human sst2 receptor
ChEMBL 338 10 2 3 4.3 NCCCCCOc1ccccc1OCCc1c[nH]c2ccccc12 10.1016/j.ejmech.2016.02.046
44354260 24077 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 674 13 5 7 4.2 CC(=O)Nc1cccc(C(=O)N2CCCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c3c[nH]c4ccccc34)C2)c1 10.1016/s0960-894x(00)00687-9
CHEMBL134043 24077 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 674 13 5 7 4.2 CC(=O)Nc1cccc(C(=O)N2CCCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c3c[nH]c4ccccc34)C2)c1 10.1016/s0960-894x(00)00687-9
44363999 40092 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 575 13 3 5 4.6 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(CCc2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL148149 40092 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 575 13 3 5 4.6 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(CCc2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
2082 2219 11 None -7079 2 Human 5.3 pKi = 5.3 Binding
Displacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST2 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting methodDisplacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST2 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 2219 11 None -7079 2 Human 5.3 pKi = 5.3 Binding
Displacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST2 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting methodDisplacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST2 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 2219 11 None -7079 2 Human 5.3 pKi = 5.3 Binding
Displacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST2 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting methodDisplacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST2 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
168275268 189555 0 None -2884 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 189555 0 None -2884 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
44354585 114993 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 621 13 4 6 4.8 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(Cc2cccc(F)c2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL335238 114993 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 621 13 4 6 4.8 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(Cc2cccc(F)c2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
44354504 116173 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 707 14 4 6 5.8 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)C(c2ccccc2)c2ccccc2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL337179 116173 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 707 14 4 6 5.8 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)C(c2ccccc2)c2ccccc2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL421362 211516 0 None 14 5 Human 8.3 pKi = 8.3 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst2) expressed in CHO-K1 cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst2) expressed 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](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm970393l
CHEMBL2369735 207908 0 None 16 5 Human 8.3 pKi = 8.3 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
91809282 125225 0 None 7 2 Human 8.3 pKi = 8.3 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 1529 23 16 14 4.4 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](Cc2c(F)c(F)c(F)c(F)c2F)NC1=O nan
CHEMBL3647683 125225 0 None 7 2 Human 8.3 pKi = 8.3 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 1529 23 16 14 4.4 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](Cc2c(F)c(F)c(F)c(F)c2F)NC1=O nan
CHEMBL2311098 207750 0 None 4 5 Human 8.3 pKi = 8.3 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
CHEMBL446077 212184 0 None 9 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned sst2 receptorBinding affinity to human cloned sst2 receptor
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
44397835 67164 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 476 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3ccc(Cl)cc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL189554 67164 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 476 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3ccc(Cl)cc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
44354298 116220 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 639 13 4 6 4.9 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(Cc2cccc(F)c2F)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL337445 116220 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 639 13 4 6 4.9 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(Cc2cccc(F)c2F)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
44364027 39211 0 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 603 14 3 5 5.5 CC(CCN1CCN([C@@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c2c[nH]c3ccccc23)C1=O)c1ccccc1 10.1016/s0960-894x(99)00016-5
CHEMBL147214 39211 0 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 603 14 3 5 5.5 CC(CCN1CCN([C@@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c2c[nH]c3ccccc23)C1=O)c1ccccc1 10.1016/s0960-894x(99)00016-5
10625454 118846 0 None -2 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 118846 0 None -2 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
CHEMBL439005 212059 0 None 1 4 Human 7.3 pKi = 7.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL2369752 207915 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
168279055 190636 0 None -4265 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 190636 0 None -4265 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
168296886 191899 0 None -5754 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 191899 0 None -5754 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
10602592 78162 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 receptor expressed in CHO-K1 cells
ChEMBL 542 10 5 4 2.9 NCCCCC(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1)C(N)=O 10.1021/jm980194h
CHEMBL2112222 78162 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 receptor expressed in CHO-K1 cells
ChEMBL 542 10 5 4 2.9 NCCCCC(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1)C(N)=O 10.1021/jm980194h
142471716 190886 0 None -1023 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 190886 0 None -1023 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
CHEMBL410181 211048 0 None -2 5 Human 6.3 pKi = 6.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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
142471841 190979 0 None -1949 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 190979 0 None -1949 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
90665463 108762 0 None -20 5 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]-somatostatin from human sst2a receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst2a 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 108762 0 None -20 5 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]-somatostatin from human sst2a receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst2a 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
CHEMBL2372956 208567 0 None 2 4 Human 7.3 pKi = 7.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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
168279197 190328 0 None -9332 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 190328 0 None -9332 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
10531093 167690 0 None -10 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 167690 0 None -10 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
168283525 190483 0 None -851 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 190483 0 None -851 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
44385757 60992 0 None -4 4 Human 5.2 pKi = 5.2 Binding
Inhibition of human sst2 receptor expressed in CHO cellsInhibition of human sst2 receptor expressed in CHO cells
ChEMBL 461 6 4 2 6.8 CC(C)(C)c1ccc(C(=N)N[C@H](Cc2c[nH]c3ccccc23)c2nc(-c3ccccc3)c[nH]2)cc1 10.1016/s0960-894x(01)00107-x
CHEMBL176730 60992 0 None -4 4 Human 5.2 pKi = 5.2 Binding
Inhibition of human sst2 receptor expressed in CHO cellsInhibition of human sst2 receptor expressed in CHO cells
ChEMBL 461 6 4 2 6.8 CC(C)(C)c1ccc(C(=N)N[C@H](Cc2c[nH]c3ccccc23)c2nc(-c3ccccc3)c[nH]2)cc1 10.1016/s0960-894x(01)00107-x
44363954 38392 0 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 in experiment 2In vitro binding affinity was evaluated against human Somatostatin receptor type 2 in experiment 2
ChEMBL 629 12 3 5 6.1 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(C2CCC(c3ccccc3)CC2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL146536 38392 0 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 in experiment 2In vitro binding affinity was evaluated against human Somatostatin receptor type 2 in experiment 2
ChEMBL 629 12 3 5 6.1 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(C2CCC(c3ccccc3)CC2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL1791307 207171 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human somatostatin receptor type 2Inhibition of human somatostatin receptor type 2
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](C)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
CHEMBL3349518 209663 0 None -10 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 2 (sst2) 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(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)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)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
CHEMBL2370168 208052 0 None 18 5 Human 8.2 pKi = 8.2 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst2) expressed in CHO-K1 cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst2) expressed in CHO-K1 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
10580397 98844 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Binding affinity for human receptor subtype hSSTR2Binding affinity for human receptor subtype hSSTR2
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 98844 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Binding affinity for human receptor subtype hSSTR2Binding affinity for human receptor subtype hSSTR2
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
71461645 78479 0 None -7 4 Human 5.2 pKi = 5.2 Binding
Inhibitory constant on human Somatostatin receptor type 2Inhibitory constant on human Somatostatin receptor type 2
ChEMBL 367 5 2 4 4.4 NCCCc1nc(-c2c[nH]c3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
CHEMBL2112935 78479 0 None -7 4 Human 5.2 pKi = 5.2 Binding
Inhibitory constant on human Somatostatin receptor type 2Inhibitory constant on human Somatostatin receptor type 2
ChEMBL 367 5 2 4 4.4 NCCCc1nc(-c2c[nH]c3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
44386389 129548 0 None -12 5 Human 5.2 pKi = 5.2 Binding
Inhibition of human sst2 receptor expressed in CHO cellsInhibition of human sst2 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 129548 0 None -12 5 Human 5.2 pKi = 5.2 Binding
Inhibition of human sst2 receptor expressed in CHO cellsInhibition of human sst2 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
44397725 123822 0 None -8 2 Human 6.2 pKi = 6.2 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 455 10 2 5 6.0 NCCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.061
CHEMBL363712 123822 0 None -8 2 Human 6.2 pKi = 6.2 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 455 10 2 5 6.0 NCCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.061
9848232 101670 0 None 6 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 receptor expressed in CHO-K1 cells
ChEMBL 485 8 4 3 3.7 NCCCCNC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/jm980194h
CHEMBL302567 101670 0 None 6 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 receptor expressed in CHO-K1 cells
ChEMBL 485 8 4 3 3.7 NCCCCNC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/jm980194h
10094509 130151 0 None -169 5 Human 5.2 pKi = 5.2 Binding
Inhibition of human sst2 receptor expressed in CHO cellsInhibition of human sst2 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 130151 0 None -169 5 Human 5.2 pKi = 5.2 Binding
Inhibition of human sst2 receptor expressed in CHO cellsInhibition of human sst2 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
9893924 4665 27 None -52 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST2 receptor expressed in HEK293 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST2 receptor expressed in HEK293 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 4665 27 None -52 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST2 receptor expressed in HEK293 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST2 receptor expressed in HEK293 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
9893924 4665 27 None -52 2 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 4665 27 None -52 2 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
168271257 189910 0 None -8912 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 189910 0 None -8912 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
CHEMBL413171 211293 0 None -5 5 Human 6.2 pKi = 6.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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
CHEMBL414598 211388 0 None -9 4 Human 6.2 pKi = 6.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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)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
142471832 189671 0 None -912 5 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 189671 0 None -912 5 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
44397834 165560 0 None -9 2 Human 6.2 pKi = 6.2 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 427 8 2 5 5.3 NCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.061
CHEMBL426072 165560 0 None -9 2 Human 6.2 pKi = 6.2 Binding
Inhibitory constant against human sst2 receptor at a dose of 10 uMInhibitory constant against human sst2 receptor at a dose of 10 uM
ChEMBL 427 8 2 5 5.3 NCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.061
127032865 138219 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]tyr11-SRIF from human sst2 receptor after 60 mins by liquid scintillation counting methodDisplacement of [125I]tyr11-SRIF from human sst2 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 138219 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]tyr11-SRIF from human sst2 receptor after 60 mins by liquid scintillation counting methodDisplacement of [125I]tyr11-SRIF from human sst2 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
CHEMBL385689 210602 0 None 2 4 Human 7.2 pKi = 7.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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(F)cc2)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL438726 212031 0 None -20 4 Human 6.2 pKi = 6.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccn2)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
142471828 191464 0 None -134 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 191464 0 None -134 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
CHEMBL1791304 207168 0 None 25 2 Human 8.2 pKi = 8.2 Binding
Inhibition of human somatostatin receptor type 2 (n=6)Inhibition of human somatostatin receptor type 2 (n=6)
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
44354587 116038 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 638 12 5 6 4.5 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)NC2CCCCC2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL336308 116038 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 638 12 5 6 4.5 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)NC2CCCCC2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
44364115 39066 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 559 8 3 5 3.7 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)NC[C@H]1OC[C@H](N)CO1)N1CCN(Cc2ccc(Cl)c(Cl)c2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL147092 39066 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 559 8 3 5 3.7 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)NC[C@H]1OC[C@H](N)CO1)N1CCN(Cc2ccc(Cl)c(Cl)c2)C1=O 10.1016/s0960-894x(99)00016-5
142471655 189821 0 None -2290 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 189821 0 None -2290 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
10816544 33573 0 None -43 2 Human 4.1 pKi = 4.1 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 33573 0 None -43 2 Human 4.1 pKi = 4.1 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
CHEMBL406738 210861 0 None 1 5 Human 7.1 pKi = 7.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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
142471891 189991 0 None -5495 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 189991 0 None -5495 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
10650940 121457 0 None -5 2 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 121457 0 None -5 2 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
10369961 34401 0 None -48 2 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 34401 0 None -48 2 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
10248767 56881 0 None -18 4 Human 5.1 pKi = 5.1 Binding
Inhibitory constant on human Somatostatin receptor type 2Inhibitory constant on human Somatostatin receptor type 2
ChEMBL 373 6 1 6 3.9 NCCCc1nc(-c2cccc([N+](=O)[O-])c2)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
CHEMBL164964 56881 0 None -18 4 Human 5.1 pKi = 5.1 Binding
Inhibitory constant on human Somatostatin receptor type 2Inhibitory constant on human Somatostatin receptor type 2
ChEMBL 373 6 1 6 3.9 NCCCc1nc(-c2cccc([N+](=O)[O-])c2)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
44364008 40264 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 595 11 3 5 4.4 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)NC[C@H]1OC[C@H](N)CO1)N1CCN(CCC(c2ccccc2)c2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL148309 40264 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 595 11 3 5 4.4 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)NC[C@H]1OC[C@H](N)CO1)N1CCN(CCC(c2ccccc2)c2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
44354462 22345 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 718 15 5 8 3.9 COC(=O)[C@H](Cc1ccccc1)NC(=O)N1CCCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c2c[nH]c3ccccc23)C1 10.1016/s0960-894x(00)00687-9
CHEMBL132610 22345 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 718 15 5 8 3.9 COC(=O)[C@H](Cc1ccccc1)NC(=O)N1CCCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c2c[nH]c3ccccc23)C1 10.1016/s0960-894x(00)00687-9
44363953 38250 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 623 12 3 5 6.2 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(c2cccc(-c3ccccc3)c2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL146431 38250 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)In vitro binding affinity was evaluated against human Somatostatin receptor type 2 (hSSTR-2)
ChEMBL 623 12 3 5 6.2 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(c2cccc(-c3ccccc3)c2)C1=O 10.1016/s0960-894x(99)00016-5
10009650 99321 0 None -7 4 Human 6.1 pKi = 6.1 Binding
Binding affinity for human receptor subtype hSSTR2Binding affinity for human receptor subtype hSSTR2
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 99321 0 None -7 4 Human 6.1 pKi = 6.1 Binding
Binding affinity for human receptor subtype hSSTR2Binding affinity for human receptor subtype hSSTR2
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
10553122 33815 0 None -1 2 Human 5.1 pKi = 5.1 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 33815 0 None -1 2 Human 5.1 pKi = 5.1 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
CHEMBL414386 211371 0 None 2 4 Human 7.1 pKi = 7.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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/jm9806289
CHEMBL2369734 207907 0 None -11 5 Human 6.1 pKi = 6.1 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
44308833 102298 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 receptor expressed in CHO-K1 cells
ChEMBL 471 7 4 3 3.3 NCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/jm980194h
CHEMBL305261 102298 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human sst2 receptor expressed in CHO-K1 cellsBinding affinity towards human sst2 receptor expressed in CHO-K1 cells
ChEMBL 471 7 4 3 3.3 NCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/jm980194h
10625762 37137 0 None 1 2 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 37137 0 None 1 2 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
CHEMBL2372962 208573 0 None 2 3 Human 7.1 pKi = 7.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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)Cc2c[nH]c3ccccc23)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O)CS1=CCCC1 10.1021/jm9806289
44354849 23932 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 618 12 4 7 3.7 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)c2cccnc2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL133909 23932 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 618 12 4 7 3.7 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)c2cccnc2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
44354851 116254 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 657 12 5 7 4.1 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)c2ccc3[nH]cnc3c2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL337645 116254 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 657 12 5 7 4.1 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCCN(C(=O)c2ccc3[nH]cnc3c2)C1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
71458043 78478 0 None -7 5 Human 5.1 pKi = 5.1 Binding
Inhibitory constant on human Somatostatin receptor type 2Inhibitory constant on human Somatostatin receptor type 2
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 78478 0 None -7 5 Human 5.1 pKi = 5.1 Binding
Inhibitory constant on human Somatostatin receptor type 2Inhibitory constant on human Somatostatin receptor type 2
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
44385652 60058 0 None -34 5 Human 5.1 pKi = 5.1 Binding
Inhibition of human sst2 receptor expressed in CHO cellsInhibition of human sst2 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 60058 0 None -34 5 Human 5.1 pKi = 5.1 Binding
Inhibition of human sst2 receptor expressed in CHO cellsInhibition of human sst2 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
CHEMBL2369751 207914 0 None 1 5 Human 7.1 pKi = 7.1 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
10602230 33730 0 None -1 2 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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 33730 0 None -1 2 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell 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
44354612 24455 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 662 13 5 7 4.7 COc1cccc(NC(=O)N2CCCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c3c[nH]c4ccccc34)C2)c1 10.1016/s0960-894x(00)00687-9
CHEMBL134353 24455 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 662 13 5 7 4.7 COc1cccc(NC(=O)N2CCCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c3c[nH]c4ccccc34)C2)c1 10.1016/s0960-894x(00)00687-9
CHEMBL2369754 207917 0 None 12 5 Human 8.0 pKi = 8.0 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 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
168280914 190198 0 None -18197 2 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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 190198 0 None -18197 2 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST2A receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST2A 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
44354503 116172 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 598 12 5 6 3.5 CC(C)NC(=O)N1CCCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c2c[nH]c3ccccc23)C1 10.1016/s0960-894x(00)00687-9
CHEMBL337178 116172 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human somatostatin 2 receptorBinding affinity to human somatostatin 2 receptor
ChEMBL 598 12 5 6 3.5 CC(C)NC(=O)N1CCCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c2c[nH]c3ccccc23)C1 10.1016/s0960-894x(00)00687-9
10096510 57112 0 None -26 4 Human 5.0 pKi = 5.0 Binding
Inhibitory constant on human Somatostatin receptor type 2Inhibitory constant on human Somatostatin receptor type 2
ChEMBL 475 7 2 6 5.2 CC(C)(C(=O)NC1CCCCC1)c1cn2cc(-c3csc4ccccc34)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
CHEMBL165402 57112 0 None -26 4 Human 5.0 pKi = 5.0 Binding
Inhibitory constant on human Somatostatin receptor type 2Inhibitory constant on human Somatostatin receptor type 2
ChEMBL 475 7 2 6 5.2 CC(C)(C(=O)NC1CCCCC1)c1cn2cc(-c3csc4ccccc34)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
CHEMBL384607 210576 0 None 1 3 Human 7.0 pKi = 7 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 2The compound was tested for binding affinity against human Somatostatin receptor type 2
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(C#N)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc(C#N)cc2)C(N)=O)NC1=O 10.1021/jm9806289
2055 2851 43 None -7 14 Mouse 8.0 pIC50 = 8.0 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2bTested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2b
Drug Central None None None None None
383414 2851 43 None -7 14 Mouse 8.0 pIC50 = 8.0 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2bTested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2b
Drug Central None None None None None
90488715 2851 43 None -7 14 Mouse 8.0 pIC50 = 8.0 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2bTested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2b
Drug Central None None None None None
CHEMBL1680 2851 43 None -7 14 Mouse 8.0 pIC50 = 8.0 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2bTested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2b
Drug Central None None None None None
CHEMBL262746 2851 43 None -7 14 Mouse 8.0 pIC50 = 8.0 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2bTested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2b
Drug Central None None None None None
DB00104 2851 43 None -7 14 Mouse 8.0 pIC50 = 8.0 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2bTested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2b
Drug Central None None None None None
16161315 214315 0 None -2 13 Mouse 8.0 pIC50 = 8.0 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2bTested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2b
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
156612990 216022 0 None - 1 Human 8.1 pKd = 8.1 Binding
Activity determined in human embryonic kidney HEK-293 cell line stably expressing human sst2 receptorsActivity determined in human embryonic kidney HEK-293 cell line stably expressing human sst2 receptors
Drug Central 1497 26 15 24 -6.0 C[C@H]([C@H]1C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=C(C=C4)O)NC(=O)[C@@H](CC5=CC=CC=C5)NC(=O)CN6CCN(CCN(CCN(CC6)CC(=O)[O-])CC(=O)[O-])CC(=O)O)C(=O)N[C@@H]([C@@H](C)O)C(=O)O)O.[64Cu+2] None
2028 1473 0 None 19 6 Human 8.5 pKd = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12616335
13105142 214317 0 125I-Tyr3-octreotide 4 5 Human 10.7 pKi = 10.7 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
16161315 214315 0 125I-Tyr3-octreotide 1 13 Human 10.5 pKi = 10.5 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 214315 0 125I-Tyr11-SRIF -2 13 Rat 10.4 pKi = 10.4 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
16161315 214315 0 125I-LTT-SST-28 1 13 Human 10.4 pKi = 10.4 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
16161315 214315 0 125I-Tyr11-SRIF-14 1 13 Human 10.5 pKi = 10.5 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
2054 3899 11 125I-Tyr3-octreotide 2 11 Human 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3899 11 125I-Tyr3-octreotide 2 11 Human 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3899 11 125I-Tyr3-octreotide 2 11 Human 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3899 11 125I-Tyr3-octreotide 2 11 Human 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3899 11 125I-Tyr3-octreotide 2 11 Human 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 214315 0 125I-Tyr11-somatostatin-14 1 13 Human 10.3 pKi = 10.3 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
None 214316 0 125I-LTT-SST-28 2 12 Human 10.3 pKi = 10.3 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 214586 0 125I-LTT-SST-28 6165 5 Human 10.3 pKi = 10.3 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 214586 0 Functional 6165 5 Human 10.3 pKi = 10.3 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 214586 0 UNDEFINED 6165 5 Human 10.3 pKi = 10.3 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
2054 3899 11 125I-SRIF-28 2 11 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3899 11 125I-SRIF-28 2 11 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3899 11 125I-SRIF-28 2 11 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3899 11 125I-SRIF-28 2 11 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3899 11 125I-SRIF-28 2 11 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 214315 0 125I-CGP23996 1 13 Human 10.2 pKi = 10.2 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
16161315 214315 0 125I-Tyr3-octreotide 1 13 Human 10.2 pKi = 10.2 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 214316 0 125I-SRIF-28 2 12 Human 10.2 pKi = 10.2 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
None 214316 0 125I-Tyr11-SRIF 2 12 Human 10.2 pKi = 10.2 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
None 214316 0 125I-Tyr11-somatostatin-14 -3 12 Mouse 10.2 pKi = 10.2 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 214315 0 125I-Tyr11-SRIF 1 13 Human 10.2 pKi = 10.2 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
16161315 214315 0 125I-Tyr11-SRIF -2 13 Rat 10.2 pKi = 10.2 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
2054 3899 11 125I-SRIF 2 11 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3899 11 125I-SRIF 2 11 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3899 11 125I-SRIF 2 11 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3899 11 125I-SRIF 2 11 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3899 11 125I-SRIF 2 11 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 214315 0 125I-Tyr10-CST14 1 13 Human 10.1 pKi = 10.1 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 214315 0 125I-Tyr11-SRIF 1 13 Human 10.1 pKi = 10.1 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 214315 0 125I-Tyr11-somatostatin-14 -2 13 Mouse 10.1 pKi = 10.1 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
None 214316 0 125I-SRIF 2 12 Human 10.1 pKi = 10.1 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
13105142 214317 0 125I-Tyr3-octreotide 4 5 Human 10.1 pKi = 10.1 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
16161315 214315 0 125I-CGP23996 1 13 Human 10.1 pKi = 10.1 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 214315 0 125I-Tyr3-octreotide 1 13 Human 10.1 pKi = 10.1 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 214315 0 125I-Tyr10-CST14 1 13 Human 10.1 pKi = 10.1 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
2054 3899 11 125I-Tyr11-SRIF -19 11 Mouse 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3899 11 125I-Tyr11-SRIF -19 11 Mouse 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3899 11 125I-Tyr11-SRIF -19 11 Mouse 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3899 11 125I-Tyr11-SRIF -19 11 Mouse 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3899 11 125I-Tyr11-SRIF -19 11 Mouse 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 214315 0 125I-LTT-SRIF28 1 13 Human 10.0 pKi = 10 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 214317 0 125I-LTT-SRIF28 4 5 Human 10.0 pKi = 10 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 214317 0 UNDEFINED 4 5 Human 10.0 pKi = 10 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 214317 0 125I-LTT-SRIF28 4 5 Human 10.0 pKi = 10.0 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 2851 43 125I-Tyr3-octreotide -1 14 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-Tyr3-octreotide -1 14 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-Tyr3-octreotide -1 14 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-Tyr3-octreotide -1 14 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-Tyr3-octreotide -1 14 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-Tyr3-octreotide -1 14 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase None None None None None
None 214316 0 125I-SOMATOSTATIN -3 12 Mouse 9.9 pKi = 9.9 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 214317 0 125I-CGP23996 4 5 Human 9.8 pKi = 9.8 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 214317 0 125I-Tyr3-octreotide 4 5 Human 9.8 pKi = 9.8 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 214316 0 125I-MK-678 -3 12 Mouse 9.7 pKi = 9.7 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 214316 0 125I-Tyr11-SRIF -3 12 Mouse 9.7 pKi = 9.7 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 214315 0 125I-SRIF-28 1 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
16161315 214315 0 125I-SOMATOSTATIN 14 1 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
16161315 214315 0 125I-SRIF 1 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
16161315 214315 0 125I-Tyr11-SRIF 1 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
16161315 214315 0 UNDEFINED 1 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
16161315 214315 0 125I-Tyr11-somatostatin-14 -2 13 Rat 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
16161315 214315 0 125I-Tyr11-somatostatin-14 1 13 Human 9.6 pKi = 9.6 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 214315 0 125I-SOMATOSTATIN -2 13 Mouse 9.6 pKi = 9.6 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
13105142 214317 0 125I-Tyr10-CST14 4 5 Human 9.6 pKi = 9.6 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 214317 0 125I-Tyr10-CST14 4 5 Human 9.6 pKi = 9.6 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 3899 11 125I-Tyr10-CST14 2 11 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3899 11 125I-Tyr10-CST14 2 11 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3899 11 125I-Tyr10-CST14 2 11 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3899 11 125I-Tyr10-CST14 2 11 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3899 11 125I-Tyr10-CST14 2 11 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 125I-LTT-SST-28 -1 14 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-LTT-SST-28 -1 14 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-LTT-SST-28 -1 14 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-LTT-SST-28 -1 14 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-LTT-SST-28 -1 14 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-LTT-SST-28 -1 14 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3899 11 125I-CGP23996 2 11 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3899 11 125I-CGP23996 2 11 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3899 11 125I-CGP23996 2 11 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3899 11 125I-CGP23996 2 11 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3899 11 125I-CGP23996 2 11 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 214315 0 125I-MK-678 -2 13 Mouse 9.6 pKi = 9.6 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 214315 0 125I-Tyr11-SRIF -2 13 Mouse 9.6 pKi = 9.6 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 214315 0 125I-Tyr11-somatostatin -2 13 Rat 9.6 pKi = 9.6 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 2851 43 125I-Tyr11-SRIF -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-Tyr11-SRIF -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-Tyr11-SRIF -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-Tyr11-SRIF -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-Tyr11-SRIF -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-Tyr11-SRIF -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
None 214316 0 125I-Tyr11-SRIF 2 12 Human 9.5 pKi = 9.5 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
2055 2851 43 125I-SRIF-28 -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-SRIF-28 -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-SRIF-28 -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-SRIF-28 -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-SRIF-28 -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-SRIF-28 -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3899 11 125I-Tyr3-octreotide 2 11 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3899 11 125I-Tyr3-octreotide 2 11 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3899 11 125I-Tyr3-octreotide 2 11 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3899 11 125I-Tyr3-octreotide 2 11 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3899 11 125I-Tyr3-octreotide 2 11 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 125I-SOMATOSTATIN 14 -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 125I-SRIF -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-SOMATOSTATIN 14 -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-SRIF -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-SOMATOSTATIN 14 -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-SRIF -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-SOMATOSTATIN 14 -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-SRIF -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-SOMATOSTATIN 14 -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-SRIF -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-SOMATOSTATIN 14 -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-SRIF -1 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 UNDEFINED -1 14 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 UNDEFINED -1 14 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 UNDEFINED -1 14 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 UNDEFINED -1 14 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 UNDEFINED -1 14 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 UNDEFINED -1 14 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3899 11 125I-LTT-SRIF28 2 11 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3899 11 125I-LTT-SRIF28 2 11 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3899 11 125I-LTT-SRIF28 2 11 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3899 11 125I-LTT-SRIF28 2 11 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3899 11 125I-LTT-SRIF28 2 11 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3899 11 125I-LTT-SRIF28 2 11 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3899 11 125I-LTT-SRIF28 2 11 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3899 11 125I-LTT-SRIF28 2 11 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3899 11 125I-LTT-SRIF28 2 11 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3899 11 125I-LTT-SRIF28 2 11 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase None None None None None
None 214316 0 125I-SOMATOSTATIN -2 12 Rat 9.3 pKi = 9.3 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 214744 0 125I-LTT-SST-28 3981 5 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2031 2232 0 UNDEFINED 2 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
71349 2232 0 UNDEFINED 2 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB06791 2232 0 UNDEFINED 2 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 125I-Tyr11-SRIF -1 14 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 125I-Tyr11-somatostatin-14 -7 14 Mouse 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-Tyr11-SRIF -1 14 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-Tyr11-somatostatin-14 -7 14 Mouse 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-Tyr11-SRIF -1 14 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-Tyr11-somatostatin-14 -7 14 Mouse 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-Tyr11-SRIF -1 14 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-Tyr11-somatostatin-14 -7 14 Mouse 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-Tyr11-SRIF -1 14 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-Tyr11-somatostatin-14 -7 14 Mouse 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-Tyr11-SRIF -1 14 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-Tyr11-somatostatin-14 -7 14 Mouse 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
None 214744 0 125I-LTT-SST-28 3981 5 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 125I-Tyr11-somatostatin-14 -1 14 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-Tyr11-somatostatin-14 -1 14 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-Tyr11-somatostatin-14 -1 14 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-Tyr11-somatostatin-14 -1 14 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-Tyr11-somatostatin-14 -1 14 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-Tyr11-somatostatin-14 -1 14 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 125I-SOMATOSTATIN -7 14 Mouse 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-SOMATOSTATIN -7 14 Mouse 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-SOMATOSTATIN -7 14 Mouse 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-SOMATOSTATIN -7 14 Mouse 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-SOMATOSTATIN -7 14 Mouse 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-SOMATOSTATIN -7 14 Mouse 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3899 11 125I-SOMATOSTATIN -19 11 Mouse 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3899 11 125I-SOMATOSTATIN -19 11 Mouse 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3899 11 125I-SOMATOSTATIN -19 11 Mouse 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3899 11 125I-SOMATOSTATIN -19 11 Mouse 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3899 11 125I-SOMATOSTATIN -19 11 Mouse 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 125I-LTT-SRIF28 -1 14 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-LTT-SRIF28 -1 14 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-LTT-SRIF28 -1 14 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-LTT-SRIF28 -1 14 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-LTT-SRIF28 -1 14 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-LTT-SRIF28 -1 14 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 125I-LTT-SRIF28 -1 14 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-LTT-SRIF28 -1 14 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-LTT-SRIF28 -1 14 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-LTT-SRIF28 -1 14 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-LTT-SRIF28 -1 14 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-LTT-SRIF28 -1 14 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 125I-CGP23996 -1 14 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-CGP23996 -1 14 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-CGP23996 -1 14 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-CGP23996 -1 14 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-CGP23996 -1 14 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-CGP23996 -1 14 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 125I-Tyr10-CST14 -1 14 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-Tyr10-CST14 -1 14 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-Tyr10-CST14 -1 14 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-Tyr10-CST14 -1 14 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-Tyr10-CST14 -1 14 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-Tyr10-CST14 -1 14 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 125I-Tyr10-CST14 -1 14 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-Tyr10-CST14 -1 14 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-Tyr10-CST14 -1 14 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-Tyr10-CST14 -1 14 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-Tyr10-CST14 -1 14 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-Tyr10-CST14 -1 14 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 125I-Tyr3-octreotide -1 14 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-Tyr3-octreotide -1 14 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-Tyr3-octreotide -1 14 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-Tyr3-octreotide -1 14 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-Tyr3-octreotide -1 14 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-Tyr3-octreotide -1 14 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3899 11 125I-SOMATOSTATIN -2 11 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3899 11 125I-SOMATOSTATIN -2 11 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3899 11 125I-SOMATOSTATIN -2 11 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3899 11 125I-SOMATOSTATIN -2 11 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3899 11 125I-SOMATOSTATIN -2 11 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 214315 0 125I-LTT-SST-28 1 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
2054 3899 11 125I-Tyr3-octreotide 2 11 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3899 11 125I-Tyr3-octreotide 2 11 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3899 11 125I-Tyr3-octreotide 2 11 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3899 11 125I-Tyr3-octreotide 2 11 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3899 11 125I-Tyr3-octreotide 2 11 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 214315 0 125I-SOMATOSTATIN -2 13 Mouse 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 214315 0 125I-SOMATOSTATIN -2 13 Rat 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
None 214585 0 125I-SOMATOSTATIN -4 9 Mouse 8.8 pKi = 8.8 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 214316 0 125I-LTT-SST-28 2 12 Human 8.8 pKi = 8.8 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 214315 0 None 1 13 Human 8.0 pKi = 8.0 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-2) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-2) subtype
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
2247 502 77 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
249 502 77 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 502 77 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 502 77 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 502 77 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 5541 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 5541 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 5542 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 5542 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 5546 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 5546 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 5587 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 5587 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 5588 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 5588 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 5590 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 5590 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 5611 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 5611 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 5624 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 5624 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 5626 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 5626 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 5631 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 5631 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 5652 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 5652 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 5654 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 5654 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 5655 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 5655 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 5670 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 5670 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 5700 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 5700 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 5711 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 5711 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 5715 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 5715 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 5716 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 5716 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 5719 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 5719 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 5749 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 5749 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 5765 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 5765 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 5766 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 5766 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 5767 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 5767 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 5829 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 5829 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 5864 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 5864 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 5971 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 5971 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 5972 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 5972 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 5973 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 5973 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 6055 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 6055 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 6056 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 6056 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 6084 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 6084 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 6123 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 6123 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 6256 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 6256 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 6257 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 6257 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 88702 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 88702 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 88703 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 88703 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 88714 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 88714 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 88715 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 88715 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 88800 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 88800 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 89263 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 89263 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 145572 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 145572 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 147336 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 147336 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 147464 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 147464 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 147808 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 147808 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 214587 0 125I-LTT-SST-28 -263 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 214587 0 UNDEFINED -263 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 215877 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 215878 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 215879 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 215880 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 215881 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 215882 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 215883 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 215884 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 215885 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 215886 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 215887 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 215888 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 215889 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
None 214585 0 125I-SOMATOSTATIN -109 9 Rat 7.0 pKi = 7 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 214585 0 125I-SOMATOSTATIN -4 9 Mouse 8.0 pKi = 8.0 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 214585 0 125I-Tyr11-somatostatin-14 -16 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 214585 0 UNDEFINED -16 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
2055 2851 43 125I-SOMATOSTATIN -10 14 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-SOMATOSTATIN -10 14 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-SOMATOSTATIN -10 14 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-SOMATOSTATIN -10 14 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-SOMATOSTATIN -10 14 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-SOMATOSTATIN -10 14 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 125I-LTT-SST-28 -1 14 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-LTT-SST-28 -1 14 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-LTT-SST-28 -1 14 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-LTT-SST-28 -1 14 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-LTT-SST-28 -1 14 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-LTT-SST-28 -1 14 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 125I-Tyr11-SRIF -7 14 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-Tyr11-SRIF -7 14 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-Tyr11-SRIF -7 14 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-Tyr11-SRIF -7 14 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-Tyr11-SRIF -7 14 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-Tyr11-SRIF -7 14 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 125I-MK-678 -7 14 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-MK-678 -7 14 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-MK-678 -7 14 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-MK-678 -7 14 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-MK-678 -7 14 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-MK-678 -7 14 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 125I-Tyr3-octreotide -1 14 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-Tyr3-octreotide -1 14 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-Tyr3-octreotide -1 14 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-Tyr3-octreotide -1 14 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-Tyr3-octreotide -1 14 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-Tyr3-octreotide -1 14 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 125I-SOMATOSTATIN -7 14 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2851 43 125I-SOMATOSTATIN -7 14 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2851 43 125I-SOMATOSTATIN -7 14 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2851 43 125I-SOMATOSTATIN -7 14 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2851 43 125I-SOMATOSTATIN -7 14 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2851 43 125I-SOMATOSTATIN -7 14 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
None 214588 0 125I-LTT-SST-28 -12589 5 Human 5.3 pKi = 5.3 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 214588 0 UNDEFINED -12589 5 Human 5.3 pKi = 5.3 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
2054 3899 11 125I-LTT-SST-28 2 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3899 11 UNDEFINED 2 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3899 11 125I-LTT-SST-28 2 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3899 11 UNDEFINED 2 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3899 11 125I-LTT-SST-28 2 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3899 11 UNDEFINED 2 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3899 11 125I-LTT-SST-28 2 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3899 11 UNDEFINED 2 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3899 11 125I-LTT-SST-28 2 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3899 11 UNDEFINED 2 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
None 214589 0 125I-LTT-SST-28 -72 5 Human 7.3 pKi = 7.3 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 214589 0 UNDEFINED -72 5 Human 7.3 pKi = 7.3 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
16161315 214315 0 125I-Tyr11-SRIF -2 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
2054 3899 11 125I-SOMATOSTATIN -19 11 Mouse 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3899 11 125I-SOMATOSTATIN -19 11 Mouse 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3899 11 125I-SOMATOSTATIN -19 11 Mouse 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3899 11 125I-SOMATOSTATIN -19 11 Mouse 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3899 11 125I-SOMATOSTATIN -19 11 Mouse 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2851 43 None -10 14 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
383414 2851 43 None -10 14 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
90488715 2851 43 None -10 14 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
CHEMBL1680 2851 43 None -10 14 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
CHEMBL262746 2851 43 None -10 14 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
DB00104 2851 43 None -10 14 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
154734381 215975 0 None -1 9 Rat 8.1 pKi = 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
None 214316 0 125I-SOMATOSTATIN -3 12 Mouse 7.1 pKi = 7.1 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
154734381 215975 0 None -1 9 Mouse 8.0 pKi = 8.0 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
154734381 215975 0 None -1 9 Human 8.0 pKi = 8.0 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
2050 2215 0 None - 1 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 585 8 5 5 4.2 NC[C@@H]1CCC[C@H](C1)CNC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 9784130
5311372 2215 0 None - 1 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 585 8 5 5 4.2 NC[C@@H]1CCC[C@H](C1)CNC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 9784130
2044 1494 0 None - 1 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2052 2694 0 None 3 2 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
15965425 2167 4 None 3090 5 Human 11.0 pKi = 11 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9724791
2046 2167 4 None 3090 5 Human 11.0 pKi = 11 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9724791
CHEMBL99895 2167 4 None 3090 5 Human 11.0 pKi = 11 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9724791
2065 232 0 None 1 2 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9804621
2067 3106 0 None 1 3 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9544214
2054 3899 11 None -19 11 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
71306 3899 11 None -19 11 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL264186 3899 11 None -19 11 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL3349523 3899 11 None -19 11 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
DB04894 3899 11 None -19 11 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2014 2175 0 None -7 9 Mouse 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2034 632 0 None 1 4 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2034 632 0 None 1 4 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2034 632 0 None 1 4 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2014 2175 0 None -5 9 Rat 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2066 3105 0 None 7 4 Rat 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9544214
2031 2232 0 None -16 9 Mouse 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
71349 2232 0 None -16 9 Mouse 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
DB06791 2232 0 None -16 9 Mouse 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2032 630 0 None -15 7 Mouse 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2029 2333 0 None 1 6 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12616335
2055 2851 43 None -7 14 Mouse 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
383414 2851 43 None -7 14 Mouse 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
90488715 2851 43 None -7 14 Mouse 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL1680 2851 43 None -7 14 Mouse 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL262746 2851 43 None -7 14 Mouse 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
DB00104 2851 43 None -7 14 Mouse 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2047 2176 0 None 1 4 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2047 2176 0 None 1 4 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2017 2693 0 None 2 3 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2004 635 0 None -3 7 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2004 635 0 None -3 7 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2004 635 0 None -3 7 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2004 635 0 None -3 7 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2051 3507 20 None -16 9 Mouse 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
5311430 3507 20 None -16 9 Mouse 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL311695 3507 20 None -16 9 Mouse 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2014 2175 0 None 2 9 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2014 2175 0 None 2 9 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2014 2175 0 None 2 9 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2035 633 0 None 3 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2055 2851 43 None -10 14 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
383414 2851 43 None -10 14 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
90488715 2851 43 None -10 14 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL1680 2851 43 None -10 14 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL262746 2851 43 None -10 14 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
DB00104 2851 43 None -10 14 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2031 2232 0 None -2 9 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
71349 2232 0 None -2 9 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
DB06791 2232 0 None -2 9 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2019 3605 0 None -13 10 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
44386062 3605 0 None -13 10 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL440072 3605 0 None -13 10 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
16133849 3606 10 None -11 9 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2020 3606 10 None -11 9 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
91935900 3606 10 None -11 9 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL501796 3606 10 None -11 9 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
16130961 876 0 None -1 6 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
16130961 876 0 None -1 6 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
16130961 876 0 None -1 6 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
16130961 876 0 None -1 6 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2005 876 0 None -1 6 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2005 876 0 None -1 6 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2005 876 0 None -1 6 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2005 876 0 None -1 6 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2054 3899 11 None -2 11 Rat 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
71306 3899 11 None -2 11 Rat 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL264186 3899 11 None -2 11 Rat 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL3349523 3899 11 None -2 11 Rat 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
DB04894 3899 11 None -2 11 Rat 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2031 2232 0 None 2 9 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2031 2232 0 None 2 9 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2031 2232 0 None 2 9 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2031 2232 0 None 2 9 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2031 2232 0 None 2 9 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
71349 2232 0 None 2 9 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
71349 2232 0 None 2 9 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
71349 2232 0 None 2 9 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
71349 2232 0 None 2 9 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
71349 2232 0 None 2 9 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
DB06791 2232 0 None 2 9 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
DB06791 2232 0 None 2 9 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
DB06791 2232 0 None 2 9 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
DB06791 2232 0 None 2 9 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
DB06791 2232 0 None 2 9 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2054 3899 11 None 2 11 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2054 3899 11 None 2 11 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
71306 3899 11 None 2 11 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
71306 3899 11 None 2 11 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL264186 3899 11 None 2 11 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL264186 3899 11 None 2 11 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL3349523 3899 11 None 2 11 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL3349523 3899 11 None 2 11 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
DB04894 3899 11 None 2 11 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
DB04894 3899 11 None 2 11 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2019 3605 0 None -5 10 Mouse 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
44386062 3605 0 None -5 10 Mouse 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL440072 3605 0 None -5 10 Mouse 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2032 630 0 None -1 7 Rat 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2038 639 0 None 3 2 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2055 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2055 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2055 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2055 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2055 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2055 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
383414 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
383414 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
383414 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
383414 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
383414 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
383414 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
90488715 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
90488715 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
90488715 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
90488715 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
90488715 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
90488715 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
CHEMBL1680 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL1680 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL1680 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL1680 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL1680 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
CHEMBL1680 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
CHEMBL262746 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL262746 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL262746 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL262746 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL262746 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
CHEMBL262746 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
DB00104 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
DB00104 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
DB00104 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
DB00104 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
DB00104 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
DB00104 2851 43 None -1 14 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
2051 3507 20 None -2 9 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
5311430 3507 20 None -2 9 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL311695 3507 20 None -2 9 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
5644 570 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8863814
2051 3507 20 None 2 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2051 3507 20 None 2 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2051 3507 20 None 2 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2051 3507 20 None 2 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2051 3507 20 None 2 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2051 3507 20 None 2 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
5311430 3507 20 None 2 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
5311430 3507 20 None 2 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
5311430 3507 20 None 2 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
5311430 3507 20 None 2 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
5311430 3507 20 None 2 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
5311430 3507 20 None 2 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
CHEMBL311695 3507 20 None 2 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL311695 3507 20 None 2 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL311695 3507 20 None 2 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL311695 3507 20 None 2 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL311695 3507 20 None 2 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
CHEMBL311695 3507 20 None 2 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
2043 1306 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2036 636 0 None -17 5 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2036 636 0 None -17 5 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2036 636 0 None -17 5 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2036 636 0 None -17 5 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2007 1143 0 None -6 6 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2007 1143 0 None -6 6 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2007 1143 0 None -6 6 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2040 641 0 None 1 4 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2008 1181 0 None -1 6 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2008 1181 0 None -1 6 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
2008 1181 0 None -1 6 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
16133849 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
16133849 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
16133849 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
16133849 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
16133849 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
16133849 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2020 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2020 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
2020 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2020 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2020 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2020 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
91935900 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
91935900 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
91935900 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
91935900 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
91935900 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
91935900 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
CHEMBL501796 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL501796 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
CHEMBL501796 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL501796 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL501796 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL501796 3606 10 None -3 9 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2048 2177 0 None - 1 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
2048 2177 0 None - 1 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
70692642 2177 0 None - 1 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
70692642 2177 0 None - 1 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
CHEMBL2052017 2177 0 None - 1 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
CHEMBL2052017 2177 0 None - 1 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
2032 630 0 None 1 7 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2037 638 0 None -1 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2019 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2019 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11520208
2019 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
2019 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2019 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2019 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2019 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2019 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
2019 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
44386062 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
44386062 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11520208
44386062 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
44386062 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
44386062 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
44386062 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
44386062 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
44386062 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
44386062 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
CHEMBL440072 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL440072 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11520208
CHEMBL440072 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
CHEMBL440072 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL440072 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL440072 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL440072 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
CHEMBL440072 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
CHEMBL440072 3605 0 None -1 10 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130