Ligand source activities (1 row/activity)





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CHEMBL1824052 215815 0 None 3 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](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
CHEMBL1824051 215814 0 None 3 5 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](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
90644981 118590 0 None 6 2 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at mouse SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 365 5 3 2 4.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287613 118590 0 None 6 2 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at mouse SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 365 5 3 2 4.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
127030549 145300 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 476 4 3 7 4.2 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL3775042 145300 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 476 4 3 7 4.2 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
90644992 118603 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 426 5 2 2 6.0 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc2ccccc2c1 10.1021/ml500079u
CHEMBL3287628 118603 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 426 5 2 2 6.0 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc2ccccc2c1 10.1021/ml500079u
CHEMBL1824056 215819 0 None 3 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay
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
CHEMBL1823873 215811 9 None -1 5 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm200307v
16129706 215810 40 None -16 12 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm200307v
CHEMBL1823872 215810 40 None -16 12 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm200307v
CHEMBL1824050 215813 0 None 3 5 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](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
10114 9334 23 None -1 6 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
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 10.1016/j.bmcl.2016.02.022
56927659 9334 23 None -1 6 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
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 10.1016/j.bmcl.2016.02.022
CHEMBL2204935 9334 23 None -1 6 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
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 10.1016/j.bmcl.2016.02.022
90644993 118604 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 444 5 2 2 6.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc2cc(F)ccc2c1 10.1021/ml500079u
CHEMBL3287629 118604 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 444 5 2 2 6.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc2cc(F)ccc2c1 10.1021/ml500079u
139392666 196981 0 None -41 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at human SST3Agonist activity at human SST3
ChEMBL 430 3 2 5 4.3 Cc1ccc(F)c2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
CHEMBL5174433 196981 0 None -41 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at human SST3Agonist activity at human SST3
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
127032341 145404 0 None - 1 Human 6.0 pEC50 = 6 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 378 2 3 3 4.5 CC(C)(C)c1c[nH]c(C2Cc3c([nH]c4ccccc34)C(C3CCOCC3)N2)n1 10.1016/j.bmcl.2016.02.022
CHEMBL3775825 145404 0 None - 1 Human 6.0 pEC50 = 6 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 378 2 3 3 4.5 CC(C)(C)c1c[nH]c(C2Cc3c([nH]c4ccccc34)C(C3CCOCC3)N2)n1 10.1016/j.bmcl.2016.02.022
122186639 129659 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 345 6 2 2 5.0 Cc1ccc(-c2c[nH]c(C3(NCCc4ccccc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605797 129659 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 345 6 2 2 5.0 Cc1ccc(-c2c[nH]c(C3(NCCc4ccccc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
90644990 118599 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 320 5 2 2 3.9 CC(C)(C)CCN[C@H]1CCCC[C@H]1NC(=O)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287622 118599 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 320 5 2 2 3.9 CC(C)(C)CCN[C@H]1CCCC[C@H]1NC(=O)c1ccc(F)cc1 10.1021/ml500079u
122186627 129647 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 370 5 3 2 5.4 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605785 129647 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 370 5 3 2 5.4 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
127032662 145333 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 454 3 3 4 6.1 c1ccc2c3c([nH]c2c1)[C@@H](C1CCOCC1)N[C@@H](c1nc(-c2csc4ccccc24)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
CHEMBL3775284 145333 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 454 3 3 4 6.1 c1ccc2c3c([nH]c2c1)[C@@H](C1CCOCC1)N[C@@H](c1nc(-c2csc4ccccc24)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
122186634 129654 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 384 6 3 2 5.5 Cc1ccc(-c2c[nH]c(C3(NCCc4c[nH]c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605792 129654 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 384 6 3 2 5.5 Cc1ccc(-c2c[nH]c(C3(NCCc4c[nH]c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
127031456 145261 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 412 3 3 3 5.2 Cc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3774791 145261 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 412 3 3 3 5.2 Cc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
122186655 129675 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 339 5 2 3 4.2 Cc1ccc(-c2c[nH]c(C3(NCC4CCOCC4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605813 129675 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 339 5 2 3 4.2 Cc1ccc(-c2c[nH]c(C3(NCC4CCOCC4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
90644983 118592 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 340 5 2 2 4.0 Cc1ccc(CN[C@H]2CCCC[C@H]2NC(=O)c2ccc(F)cc2)cc1 10.1021/ml500079u
CHEMBL3287615 118592 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 340 5 2 2 4.0 Cc1ccc(CN[C@H]2CCCC[C@H]2NC(=O)c2ccc(F)cc2)cc1 10.1021/ml500079u
90644985 118594 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 356 6 2 3 3.7 COc1ccc(CN[C@H]2CCCC[C@H]2NC(=O)c2ccc(F)cc2)cc1 10.1021/ml500079u
CHEMBL3287617 118594 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 356 6 2 3 3.7 COc1ccc(CN[C@H]2CCCC[C@H]2NC(=O)c2ccc(F)cc2)cc1 10.1021/ml500079u
90644998 118616 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 379 5 2 2 4.5 CN(Cc1c[nH]c2ccccc12)[C@H]1CCCC[C@H]1NC(=O)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287643 118616 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 379 5 2 2 4.5 CN(Cc1c[nH]c2ccccc12)[C@H]1CCCC[C@H]1NC(=O)c1ccc(F)cc1 10.1021/ml500079u
90644997 118611 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 369 5 3 2 3.9 O=C(N[C@@H]1CCC[C@H]1NCc1c[nH]c2ccccc12)c1ccc(F)c(F)c1 10.1021/ml500079u
CHEMBL3287635 118611 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 369 5 3 2 3.9 O=C(N[C@@H]1CCC[C@H]1NCc1c[nH]c2ccccc12)c1ccc(F)c(F)c1 10.1021/ml500079u
127032661 145303 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 418 3 3 4 5.3 Cc1csc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
CHEMBL3775055 145303 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 418 3 3 4 5.3 Cc1csc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
122186653 129673 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 382 5 2 3 5.5 Cc1ccc(-c2c[nH]c(C3(NCc4ccc5ncccc5c4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605811 129673 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 382 5 2 3 5.5 Cc1ccc(-c2c[nH]c(C3(NCc4ccc5ncccc5c4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
122186637 129657 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 370 5 3 2 5.4 Cc1ccc(-c2c[nH]c(C3(NCc4cc5ccccc5[nH]4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605795 129657 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 370 5 3 2 5.4 Cc1ccc(-c2c[nH]c(C3(NCc4cc5ccccc5[nH]4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL1824049 215812 0 None 1 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](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
127033870 145311 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 430 3 2 4 5.1 Cn1c2c(c3ccccc31)C[C@H](c1nc(-c3ccc(F)cc3)c[nH]1)N[C@@H]2C1CCOCC1 10.1016/j.bmcl.2016.02.022
CHEMBL3775120 145311 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 430 3 2 4 5.1 Cn1c2c(c3ccccc31)C[C@H](c1nc(-c3ccc(F)cc3)c[nH]1)N[C@@H]2C1CCOCC1 10.1016/j.bmcl.2016.02.022
127030226 145399 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 466 3 3 3 5.9 FC(F)(F)c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775793 145399 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 466 3 3 3 5.9 FC(F)(F)c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
90644988 118597 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 370 6 3 3 3.4 O=C(O)c1ccc(CN[C@H]2CCCC[C@H]2NC(=O)c2ccc(F)cc2)cc1 10.1021/ml500079u
CHEMBL3287620 118597 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 370 6 3 3 3.4 O=C(O)c1ccc(CN[C@H]2CCCC[C@H]2NC(=O)c2ccc(F)cc2)cc1 10.1021/ml500079u
122186626 129646 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 356 5 3 2 5.0 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605784 129646 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 356 5 3 2 5.0 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
122186643 129663 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 337 5 2 2 4.7 Cc1ccc(-c2c[nH]c(C3(NCCC(F)(F)F)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605801 129663 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 337 5 2 2 4.7 Cc1ccc(-c2c[nH]c(C3(NCCC(F)(F)F)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL1824057 215820 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Partial agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assayPartial agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2cn(Cc3ccccc3)cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm200307v
127030229 145296 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 428 4 3 4 4.9 COc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
CHEMBL3775031 145296 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 428 4 3 4 4.9 COc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
127033002 145315 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 507 5 3 9 3.6 COc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@](c4cnn(C)c4)(c4noc(C)n4)N3)n2)n1 10.1016/j.bmcl.2016.02.022
CHEMBL3775160 145315 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 507 5 3 9 3.6 COc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@](c4cnn(C)c4)(c4noc(C)n4)N3)n2)n1 10.1016/j.bmcl.2016.02.022
127034125 145390 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 412 3 3 3 5.1 CC1(c2nc(-c3ccccc3)c[nH]2)Cc2c([nH]c3ccccc23)C(C2CCOCC2)N1 10.1016/j.bmcl.2016.02.022
CHEMBL3775729 145390 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 412 3 3 3 5.1 CC1(c2nc(-c3ccccc3)c[nH]2)Cc2c([nH]c3ccccc23)C(C2CCOCC2)N1 10.1016/j.bmcl.2016.02.022
122186645 129665 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 365 5 2 2 5.6 Cc1ccc(-c2c[nH]c(C3(NCc4ccc(Cl)cc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605803 129665 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 365 5 2 2 5.6 Cc1ccc(-c2c[nH]c(C3(NCc4ccc(Cl)cc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
127030228 145332 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 428 4 3 4 4.9 COc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775282 145332 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 428 4 3 4 4.9 COc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
127033551 145351 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 399 3 3 4 4.3 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)nc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775418 145351 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 399 3 3 4 4.3 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)nc1 10.1016/j.bmcl.2016.02.022
127030548 145280 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 433 3 3 4 5.0 Clc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)nc1 10.1016/j.bmcl.2016.02.022
CHEMBL3774909 145280 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 433 3 3 4 5.0 Clc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)nc1 10.1016/j.bmcl.2016.02.022
122179457 128232 0 None 794 4 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 495 4 3 8 3.7 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL3582317 128232 0 None 794 4 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 495 4 3 8 3.7 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
90644981 118590 0 None -6 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 365 5 3 2 4.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287613 118590 0 None -6 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 365 5 3 2 4.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
122186630 129650 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 356 5 3 2 5.1 c1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605788 129650 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 356 5 3 2 5.1 c1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
122186635 129655 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 371 5 3 3 4.8 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5cccnc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605793 129655 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 371 5 3 3 4.8 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5cccnc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
90644978 118620 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 365 5 3 2 4.6 O=C(Nc1ccc(F)cc1)[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12 10.1021/ml500079u
CHEMBL3287649 118620 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 365 5 3 2 4.6 O=C(Nc1ccc(F)cc1)[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12 10.1021/ml500079u
127033874 145378 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 417 3 3 4 4.4 Fc1ccc(-c2n[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775625 145378 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 417 3 3 4 4.4 Fc1ccc(-c2n[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
127032660 145353 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 438 3 3 4 5.6 Clc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)s1 10.1016/j.bmcl.2016.02.022
CHEMBL3775435 145353 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 438 3 3 4 5.6 Clc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)s1 10.1016/j.bmcl.2016.02.022
90644984 118593 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 344 5 2 2 3.8 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(F)cc1)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287616 118593 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 344 5 2 2 3.8 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(F)cc1)c1ccc(F)cc1 10.1021/ml500079u
90644995 118607 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 426 5 2 2 6.0 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1cccc2ccccc12 10.1021/ml500079u
CHEMBL3287631 118607 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 426 5 2 2 6.0 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1cccc2ccccc12 10.1021/ml500079u
57384077 83622 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL2069502 83622 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
122186652 129672 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 407 6 2 2 6.6 Cc1ccc(-c2c[nH]c(C3(NCc4ccc(-c5ccccc5)cc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605810 129672 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 407 6 2 2 6.6 Cc1ccc(-c2c[nH]c(C3(NCc4ccc(-c5ccccc5)cc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
122186629 129649 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 385 5 4 3 4.2 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCNCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605787 129649 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 385 5 4 3 4.2 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCNCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
90644987 118596 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 397 8 2 3 4.5 CCN(CC)c1ccc(CN[C@H]2CCCC[C@H]2NC(=O)c2ccc(F)cc2)cc1 10.1021/ml500079u
CHEMBL3287619 118596 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 397 8 2 3 4.5 CCN(CC)c1ccc(CN[C@H]2CCCC[C@H]2NC(=O)c2ccc(F)cc2)cc1 10.1021/ml500079u
90644994 118606 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 427 5 2 3 5.4 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc2ccccc2n1 10.1021/ml500079u
CHEMBL3287630 118606 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 427 5 2 3 5.4 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc2ccccc2n1 10.1021/ml500079u
122186647 129667 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 349 5 2 2 5.1 Cc1ccc(-c2c[nH]c(C3(NCc4ccc(F)cc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605805 129667 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 349 5 2 2 5.1 Cc1ccc(-c2c[nH]c(C3(NCc4ccc(F)cc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
127030227 145346 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 414 3 4 4 4.6 Oc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775398 145346 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 414 3 4 4 4.6 Oc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
122186632 129652 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 432 6 3 2 6.8 c1ccc(-c2ccc(-c3c[nH]c(C4(NCc5c[nH]c6ccccc56)CCCC4)n3)cc2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605790 129652 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 432 6 3 2 6.8 c1ccc(-c2ccc(-c3c[nH]c(C4(NCc5c[nH]c6ccccc56)CCCC4)n3)cc2)cc1 10.1016/j.bmcl.2015.06.087
90644977 118619 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 410 5 2 3 5.8 O=C(Nc1ccc(F)cc1)O[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1 10.1021/ml500079u
CHEMBL3287648 118619 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 410 5 2 3 5.8 O=C(Nc1ccc(F)cc1)O[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1 10.1021/ml500079u
CHEMBL1824058 215821 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Partial agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assayPartial agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2cn(Cc3ccccc3)cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm200307v
127031432 145344 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 429 4 3 5 4.3 COc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)n1 10.1016/j.bmcl.2016.02.022
CHEMBL3775387 145344 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 429 4 3 5 4.3 COc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)n1 10.1016/j.bmcl.2016.02.022
127030550 145379 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 476 4 3 7 4.2 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL3775630 145379 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 476 4 3 7 4.2 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL452157 220755 0 None -3 5 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay
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
90644996 118608 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 365 5 3 2 4.1 O=C(N[C@@H]1CCCC[C@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287632 118608 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 365 5 3 2 4.1 O=C(N[C@@H]1CCCC[C@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
127031155 145226 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 416 3 3 3 5.1 Fc1ccccc1-c1c[nH]c([C@H]2Cc3c([nH]c4ccccc34)[C@@H](C3CCOCC3)N2)n1 10.1016/j.bmcl.2016.02.022
CHEMBL3774495 145226 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 416 3 3 3 5.1 Fc1ccccc1-c1c[nH]c([C@H]2Cc3c([nH]c4ccccc34)[C@@H](C3CCOCC3)N2)n1 10.1016/j.bmcl.2016.02.022
CHEMBL1824053 215816 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Partial agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assayPartial agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](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
90644999 118622 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 365 5 3 2 4.1 O=C(N[C@H]1CCCC[C@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287651 118622 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 365 5 3 2 4.1 O=C(N[C@H]1CCCC[C@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
122186654 129674 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 337 5 2 2 5.3 Cc1ccc(-c2c[nH]c(C3(NCC4CCCCC4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605812 129674 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 337 5 2 2 5.3 Cc1ccc(-c2c[nH]c(C3(NCC4CCCCC4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
90644979 118621 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 365 5 3 2 4.6 O=C(Nc1ccc(F)cc1)[C@@H]1CCCC[C@H]1NCc1c[nH]c2ccccc12 10.1021/ml500079u
CHEMBL3287650 118621 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 365 5 3 2 4.6 O=C(Nc1ccc(F)cc1)[C@@H]1CCCC[C@H]1NCc1c[nH]c2ccccc12 10.1021/ml500079u
122186642 129662 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 325 5 2 2 5.2 Cc1ccc(-c2c[nH]c(C3(NCCC(C)(C)C)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605800 129662 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 325 5 2 2 5.2 Cc1ccc(-c2c[nH]c(C3(NCCC(C)(C)C)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
90644986 118595 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 342 5 3 3 3.4 O=C(N[C@@H]1CCCC[C@@H]1NCc1cccc(O)c1)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287618 118595 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 342 5 3 3 3.4 O=C(N[C@@H]1CCCC[C@@H]1NCc1cccc(O)c1)c1ccc(F)cc1 10.1021/ml500079u
127030231 145301 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 434 3 3 3 5.2 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c(F)c1 10.1016/j.bmcl.2016.02.022
CHEMBL3775050 145301 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 434 3 3 3 5.2 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c(F)c1 10.1016/j.bmcl.2016.02.022
122186646 129666 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 399 5 2 2 6.0 Cc1ccc(-c2c[nH]c(C3(NCc4ccc(C(F)(F)F)cc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605804 129666 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 399 5 2 2 6.0 Cc1ccc(-c2c[nH]c(C3(NCc4ccc(C(F)(F)F)cc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
122186656 129676 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 335 5 2 4 3.7 Cc1ccc(-c2c[nH]c(C3(NCc4cnn(C)c4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605814 129676 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 335 5 2 4 3.7 Cc1ccc(-c2c[nH]c(C3(NCc4cnn(C)c4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
122186636 129656 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 400 6 3 3 5.4 COc1cccc2c(CNC3(c4nc(-c5ccc(C)cc5)c[nH]4)CCCC3)c[nH]c12 10.1016/j.bmcl.2015.06.087
CHEMBL3605794 129656 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 400 6 3 3 5.4 COc1cccc2c(CNC3(c4nc(-c5ccc(C)cc5)c[nH]4)CCCC3)c[nH]c12 10.1016/j.bmcl.2015.06.087
139392804 198382 1 None -104 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST3Agonist activity at human SST3
ChEMBL 412 3 2 5 4.1 Cc1cccc2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
CHEMBL5195355 198382 1 None -104 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST3Agonist activity at human SST3
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
122186624 129644 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 344 5 3 2 4.9 Cc1ccc(-c2c[nH]c(C(C)(C)NCc3c[nH]c4ccccc34)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605782 129644 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 344 5 3 2 4.9 Cc1ccc(-c2c[nH]c(C(C)(C)NCc3c[nH]c4ccccc34)n2)cc1 10.1016/j.bmcl.2015.06.087
90644991 118602 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 412 5 2 2 5.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc(F)c(F)c1 10.1021/ml500079u
CHEMBL3287627 118602 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 412 5 2 2 5.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc(F)c(F)c1 10.1021/ml500079u
CHEMBL1824055 215818 0 None -10 5 Human 8.3 pEC50 = 8.3 Functional
Partial agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assayPartial agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay
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
127034429 145251 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 507 5 3 9 3.6 COc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@](c4cnn(C)c4)(c4noc(C)n4)N3)n2)n1 10.1016/j.bmcl.2016.02.022
CHEMBL3774684 145251 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 507 5 3 9 3.6 COc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@](c4cnn(C)c4)(c4noc(C)n4)N3)n2)n1 10.1016/j.bmcl.2016.02.022
127033873 145299 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 398 3 3 3 4.9 c1ccc(-c2nc([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)c[nH]2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775037 145299 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 398 3 3 3 4.9 c1ccc(-c2nc([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)c[nH]2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL1824054 215817 0 None 4 2 Human 7.4 pEC50 = 7.4 Functional
Partial agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assayPartial agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](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
122186649 129669 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 332 5 2 3 4.3 Cc1ccc(-c2c[nH]c(C3(NCc4ccncc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605807 129669 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 332 5 2 3 4.3 Cc1ccc(-c2c[nH]c(C3(NCc4ccncc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
122186657 129677 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 349 6 2 4 4.2 CCn1cncc1CNC1(c2nc(-c3ccc(C)cc3)c[nH]2)CCCC1 10.1016/j.bmcl.2015.06.087
CHEMBL3605815 129677 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 349 6 2 4 4.2 CCn1cncc1CNC1(c2nc(-c3ccc(C)cc3)c[nH]2)CCCC1 10.1016/j.bmcl.2015.06.087
122186628 129648 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 384 5 3 2 5.8 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605786 129648 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 384 5 3 2 5.8 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
127031464 145279 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 399 3 3 4 4.3 c1ccc2c3c([nH]c2c1)[C@@H](C1CCOCC1)N[C@@H](c1nc(-c2ccncc2)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
CHEMBL3774903 145279 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 399 3 3 4 4.3 c1ccc2c3c([nH]c2c1)[C@@H](C1CCOCC1)N[C@@H](c1nc(-c2ccncc2)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
127033555 145326 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 423 3 3 4 4.8 N#Cc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
CHEMBL3775241 145326 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 423 3 3 4 4.8 N#Cc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
127031771 145292 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 400 3 3 5 3.7 c1ccc2c3c([nH]c2c1)[C@@H](C1CCOCC1)N[C@@H](c1nc(-c2cnccn2)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
CHEMBL3775018 145292 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 400 3 3 5 3.7 c1ccc2c3c([nH]c2c1)[C@@H](C1CCOCC1)N[C@@H](c1nc(-c2cnccn2)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
127032659 145244 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 404 3 3 4 5.0 c1ccc2c3c([nH]c2c1)[C@@H](C1CCOCC1)N[C@@H](c1nc(-c2ccsc2)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
CHEMBL3774626 145244 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 404 3 3 4 5.0 c1ccc2c3c([nH]c2c1)[C@@H](C1CCOCC1)N[C@@H](c1nc(-c2ccsc2)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
122186650 129670 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 333 5 2 4 3.7 Cc1ccc(-c2c[nH]c(C3(NCc4cncnc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605808 129670 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 333 5 2 4 3.7 Cc1ccc(-c2c[nH]c(C3(NCc4cncnc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
122186640 129660 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 359 7 2 2 5.4 Cc1ccc(-c2c[nH]c(C3(NCCCc4ccccc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605798 129660 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 359 7 2 2 5.4 Cc1ccc(-c2c[nH]c(C3(NCCCc4ccccc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
127034426 145394 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 477 4 3 8 3.6 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccccn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL3775760 145394 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 477 4 3 8 3.6 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccccn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
71452299 90437 0 None 1 2 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 416 3 3 3 5.1 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL2204941 90437 0 None 1 2 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 416 3 3 3 5.1 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
127031454 145273 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 432 3 3 3 5.6 Clc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3774866 145273 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 432 3 3 3 5.6 Clc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
122186633 129653 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 384 5 2 3 5.4 Cc1ccc(-c2c[nH]c(C3(NCc4cn(C)c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605791 129653 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 384 5 2 3 5.4 Cc1ccc(-c2c[nH]c(C3(NCc4cn(C)c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
90644989 118598 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 354 7 2 2 4.1 O=C(N[C@@H]1CCCC[C@@H]1NCCCc1ccccc1)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287621 118598 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 354 7 2 2 4.1 O=C(N[C@@H]1CCCC[C@@H]1NCCCc1ccccc1)c1ccc(F)cc1 10.1021/ml500079u
90644982 118591 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 394 5 2 2 5.0 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287614 118591 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 394 5 2 2 5.0 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc(F)cc1 10.1021/ml500079u
127030230 145361 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 434 3 3 3 5.2 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1F 10.1016/j.bmcl.2016.02.022
CHEMBL3775532 145361 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 434 3 3 3 5.2 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1F 10.1016/j.bmcl.2016.02.022
122186638 129658 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 331 5 2 2 4.9 Cc1ccc(-c2c[nH]c(C3(NCc4ccccc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605796 129658 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 331 5 2 2 4.9 Cc1ccc(-c2c[nH]c(C3(NCc4ccccc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
127030547 145391 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 417 3 3 4 4.4 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)nc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775734 145391 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 417 3 3 4 4.4 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)nc1 10.1016/j.bmcl.2016.02.022
127032340 145369 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 404 3 3 3 5.3 c1ccc2c3c([nH]c2c1)C(C1CCOCC1)NC(c1nc(C2CCCCC2)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
CHEMBL3775580 145369 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 404 3 3 3 5.3 c1ccc2c3c([nH]c2c1)C(C1CCOCC1)NC(c1nc(C2CCCCC2)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
127034428 145304 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 495 4 3 8 3.7 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL3775061 145304 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 495 4 3 8 3.7 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
127034427 145264 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 477 4 3 8 3.6 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccccn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL3774800 145264 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 477 4 3 8 3.6 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccccn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
122186641 129661 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 283 5 2 2 4.2 CCCNC1(c2nc(-c3ccc(C)cc3)c[nH]2)CCCC1 10.1016/j.bmcl.2015.06.087
CHEMBL3605799 129661 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 283 5 2 2 4.2 CCCNC1(c2nc(-c3ccc(C)cc3)c[nH]2)CCCC1 10.1016/j.bmcl.2015.06.087
122186631 129651 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 374 5 3 2 5.3 Fc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605789 129651 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 374 5 3 2 5.3 Fc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
127031154 145266 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 416 3 3 3 5.1 Fc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
CHEMBL3774817 145266 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 416 3 3 3 5.1 Fc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
90644976 118618 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 409 5 3 2 5.4 O=C(Nc1ccc(F)cc1)N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1 10.1021/ml500079u
CHEMBL3287647 118618 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 409 5 3 2 5.4 O=C(Nc1ccc(F)cc1)N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1 10.1021/ml500079u
122186648 129668 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 349 5 2 2 5.1 Cc1ccc(-c2c[nH]c(C3(NCc4cccc(F)c4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605806 129668 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 349 5 2 2 5.1 Cc1ccc(-c2c[nH]c(C3(NCc4cccc(F)c4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
127033872 145415 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 416 3 3 3 5.1 Fc1ccc(-c2cc([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)[nH]n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775922 145415 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levelsAntagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels
ChEMBL 416 3 3 3 5.1 Fc1ccc(-c2cc([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)[nH]n2)cc1 10.1016/j.bmcl.2016.02.022
3156873 118614 9 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 311 6 3 2 2.8 O=C(NCCNCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287639 118614 9 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAgonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 311 6 3 2 2.8 O=C(NCCNCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
122186644 129664 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 361 6 2 3 5.0 COc1ccc(CNC2(c3nc(-c4ccc(C)cc4)c[nH]3)CCCC2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605802 129664 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 361 6 2 3 5.0 COc1ccc(CNC2(c3nc(-c4ccc(C)cc4)c[nH]3)CCCC2)cc1 10.1016/j.bmcl.2015.06.087
122186651 129671 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 389 6 2 4 4.7 COC(=O)c1ccc(CNC2(c3nc(-c4ccc(C)cc4)c[nH]3)CCCC2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605809 129671 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assayAgonist activity at human SSTR3 expressed in CHO cells assessed as intracellular cAMP level after 45 mins by time-resolved fluorescence assay
ChEMBL 389 6 2 4 4.7 COC(=O)c1ccc(CNC2(c3nc(-c4ccc(C)cc4)c[nH]3)CCCC2)cc1 10.1016/j.bmcl.2015.06.087
71462983 90434 0 None 3 2 Mouse 9.9 pIC50 = 9.9 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@]2(c3cnn(C)c3)N[C@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204938 90434 0 None 3 2 Mouse 9.9 pIC50 = 9.9 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@]2(c3cnn(C)c3)N[C@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
118710527 120474 0 None 1 2 Human 9.8 pIC50 = 9.8 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cncc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
CHEMBL3323076 120474 0 None 1 2 Human 9.8 pIC50 = 9.8 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cncc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
118710534 120482 0 None 5 2 Mouse 9.8 pIC50 = 9.8 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cncc(C(=O)O)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323084 120482 0 None 5 2 Mouse 9.8 pIC50 = 9.8 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cncc(C(=O)O)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
122179483 128261 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 568 7 4 10 2.1 CCn1cc([C@@]2(c3nn(CC(N)=O)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582344 128261 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 568 7 4 10 2.1 CCn1cc([C@@]2(c3nn(CC(N)=O)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
118710527 120474 0 None -1 2 Mouse 9.5 pIC50 = 9.5 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cncc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
CHEMBL3323076 120474 0 None -1 2 Mouse 9.5 pIC50 = 9.5 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cncc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
118710525 120472 0 None 1 2 Mouse 9.4 pIC50 = 9.4 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccnc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
CHEMBL3323074 120472 0 None 1 2 Mouse 9.4 pIC50 = 9.4 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccnc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
122179461 128237 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 535 6 3 8 4.6 Cc1nc([C@]2(c3cnn(CC4CC4)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml500514w
CHEMBL3582321 128237 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 535 6 3 8 4.6 Cc1nc([C@]2(c3cnn(CC4CC4)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml500514w
122179478 128255 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 539 6 3 9 3.7 CCn1cc([C@@]2(c3nn(CC)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582339 128255 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 539 6 3 9 3.7 CCn1cc([C@@]2(c3nn(CC)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
10114 9334 23 None 1 6 Mouse 9.3 pIC50 = 9.3 Functional
Antagonist activity at mouse SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAntagonist activity at mouse SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
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/ml500079u
56927659 9334 23 None 1 6 Mouse 9.3 pIC50 = 9.3 Functional
Antagonist activity at mouse SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAntagonist activity at mouse SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
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/ml500079u
CHEMBL2204935 9334 23 None 1 6 Mouse 9.3 pIC50 = 9.3 Functional
Antagonist activity at mouse SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAntagonist activity at mouse SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
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/ml500079u
10114 9334 23 None 1 6 Mouse 9.3 pIC50 = 9.3 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 494 4 3 7 4.3 Fc1ccc(cc1)c1cnc([nH]1)[C@H]1Cc2c3ccccc3[nH]c2[C@@](N1)(c1noc(n1)C)c1cnn(c1)C 10.1021/ml300063m
56927659 9334 23 None 1 6 Mouse 9.3 pIC50 = 9.3 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 494 4 3 7 4.3 Fc1ccc(cc1)c1cnc([nH]1)[C@H]1Cc2c3ccccc3[nH]c2[C@@](N1)(c1noc(n1)C)c1cnn(c1)C 10.1021/ml300063m
CHEMBL2204935 9334 23 None 1 6 Mouse 9.3 pIC50 = 9.3 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 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
71459516 90435 0 None 1 2 Mouse 9.3 pIC50 = 9.3 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 492 4 3 6 4.3 Cn1cc(C2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
CHEMBL2204939 90435 0 None 1 2 Mouse 9.3 pIC50 = 9.3 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 492 4 3 6 4.3 Cn1cc(C2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
122179481 128259 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 582 8 3 10 3.2 CCn1cc([C@@]2(c3nn(CCN(C)C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582342 128259 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 582 8 3 10 3.2 CCn1cc([C@@]2(c3nn(CCN(C)C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
118710534 120482 0 None -5 2 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cncc(C(=O)O)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323084 120482 0 None -5 2 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cncc(C(=O)O)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
118710523 120470 0 None 2 2 Mouse 9.2 pIC50 = 9.2 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cccc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)n1 10.1021/ml500028c
CHEMBL3323072 120470 0 None 2 2 Mouse 9.2 pIC50 = 9.2 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cccc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)n1 10.1021/ml500028c
122179469 128245 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 541 6 3 9 4.6 CCn1cc([C@@]2(c3nnc(SC)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582329 128245 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 541 6 3 9 4.6 CCn1cc([C@@]2(c3nnc(SC)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
71459516 90435 0 None -1 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 492 4 3 6 4.3 Cn1cc(C2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
CHEMBL2204939 90435 0 None -1 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 492 4 3 6 4.3 Cn1cc(C2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
86279005 120480 2 None 1 2 Mouse 9.1 pIC50 = 9.1 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cc(C(=O)O)ccn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323082 120480 2 None 1 2 Mouse 9.1 pIC50 = 9.1 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cc(C(=O)O)ccn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
118710525 120472 0 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccnc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
CHEMBL3323074 120472 0 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccnc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
71462983 90434 0 None -3 2 Human 9.1 pIC50 = 9.1 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@]2(c3cnn(C)c3)N[C@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204938 90434 0 None -3 2 Human 9.1 pIC50 = 9.1 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@]2(c3cnn(C)c3)N[C@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
122179476 128251 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 539 5 3 9 3.7 CC(C)n1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)oc1=O 10.1021/ml500514w
CHEMBL3582335 128251 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 539 5 3 9 3.7 CC(C)n1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)oc1=O 10.1021/ml500514w
122179482 128260 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 569 7 4 10 2.7 CCn1cc([C@@]2(c3nn(CC(=O)O)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582343 128260 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 569 7 4 10 2.7 CCn1cc([C@@]2(c3nn(CC(=O)O)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
73348311 96007 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.
ChEMBL 454 10 3 2 7.8 CCCCCC1(CCCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL2367837 96007 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.
ChEMBL 454 10 3 2 7.8 CCCCCC1(CCCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
10114 9334 23 None -1 6 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
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/ml500514w
56927659 9334 23 None -1 6 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
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/ml500514w
CHEMBL2204935 9334 23 None -1 6 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
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/ml500514w
10114 9334 23 None -1 6 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAntagonist activity at human SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
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/ml500079u
56927659 9334 23 None -1 6 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAntagonist activity at human SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
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/ml500079u
CHEMBL2204935 9334 23 None -1 6 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAntagonist activity at human SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
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/ml500079u
10114 9334 23 None -1 6 Human 9.0 pIC50 = 9.0 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 494 4 3 7 4.3 Fc1ccc(cc1)c1cnc([nH]1)[C@H]1Cc2c3ccccc3[nH]c2[C@@](N1)(c1noc(n1)C)c1cnn(c1)C 10.1021/ml300063m
56927659 9334 23 None -1 6 Human 9.0 pIC50 = 9.0 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 494 4 3 7 4.3 Fc1ccc(cc1)c1cnc([nH]1)[C@H]1Cc2c3ccccc3[nH]c2[C@@](N1)(c1noc(n1)C)c1cnn(c1)C 10.1021/ml300063m
CHEMBL2204935 9334 23 None -1 6 Human 9.0 pIC50 = 9.0 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 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
122179479 128257 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 553 6 3 9 4.2 CCn1cc([C@@]2(c3nn(C(C)C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582340 128257 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 553 6 3 9 4.2 CCn1cc([C@@]2(c3nn(C(C)C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
122179477 128252 5 None -2 7 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 525 5 3 9 3.2 CCn1cc([C@@]2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582336 128252 5 None -2 7 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 525 5 3 9 3.2 CCn1cc([C@@]2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
71454093 90432 0 None 1 2 Human 9.0 pIC50 = 9.0 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204936 90432 0 None 1 2 Human 9.0 pIC50 = 9.0 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
122179459 128234 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 509 5 3 8 4.2 CCn1cc([C@@]2(c3noc(C)n3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582319 128234 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 509 5 3 8 4.2 CCn1cc([C@@]2(c3noc(C)n3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
122179460 128236 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 509 5 3 8 4.0 CCc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml500514w
CHEMBL3582320 128236 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 509 5 3 8 4.0 CCc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml500514w
71461260 90436 0 None -1 2 Human 8.9 pIC50 = 8.9 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 496 4 3 8 4.3 Cc1nc(C2(c3noc(C)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204940 90436 0 None -1 2 Human 8.9 pIC50 = 8.9 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 496 4 3 8 4.3 Cc1nc(C2(c3noc(C)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
122179480 128258 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 565 7 3 9 4.0 CCn1cc([C@@]2(c3nn(CC4CC4)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582341 128258 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 565 7 3 9 4.0 CCn1cc([C@@]2(c3nn(CC4CC4)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
71461260 90436 0 None 1 2 Mouse 8.9 pIC50 = 8.9 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 496 4 3 8 4.3 Cc1nc(C2(c3noc(C)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204940 90436 0 None 1 2 Mouse 8.9 pIC50 = 8.9 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 496 4 3 8 4.3 Cc1nc(C2(c3noc(C)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
118710529 120476 0 None 1 2 Mouse 8.8 pIC50 = 8.8 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)nc1 10.1021/ml500028c
CHEMBL3323078 120476 0 None 1 2 Mouse 8.8 pIC50 = 8.8 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)nc1 10.1021/ml500028c
122179475 128085 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 525 5 3 9 3.2 CCn1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)oc1=O 10.1021/ml500514w
CHEMBL3580681 128085 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 525 5 3 9 3.2 CCn1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)oc1=O 10.1021/ml500514w
86279005 120480 2 None -1 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cc(C(=O)O)ccn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323082 120480 2 None -1 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cc(C(=O)O)ccn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
118710523 120470 0 None -2 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cccc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)n1 10.1021/ml500028c
CHEMBL3323072 120470 0 None -2 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cccc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)n1 10.1021/ml500028c
70688791 83625 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 414 3 3 3 5.6 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCSCC4)N3)n2)cc1 10.1021/ml200272z
CHEMBL2069505 83625 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 414 3 3 3 5.6 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCSCC4)N3)n2)cc1 10.1021/ml200272z
70682466 83628 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 497 3 3 4 6.1 CC(C)(C)OC(=O)N1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL2069508 83628 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 497 3 3 4 6.1 CC(C)(C)OC(=O)N1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
118710532 120479 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3cccc(C(=O)O)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323081 120479 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3cccc(C(=O)O)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
122179458 128233 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 481 4 4 7 3.7 Cc1nc([C@]2(c3cn[nH]c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml500514w
CHEMBL3582318 128233 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 481 4 4 7 3.7 Cc1nc([C@]2(c3cn[nH]c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml500514w
57384077 83622 0 None -1 2 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml300063m
CHEMBL2069502 83622 0 None -1 2 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml300063m
122179463 128239 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 510 5 4 9 2.8 Cn1cc([C@@]2(c3noc(CN)n3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582323 128239 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 510 5 4 9 2.8 Cn1cc([C@@]2(c3noc(CN)n3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
118710532 120479 0 None -1 2 Mouse 7.0 pIC50 = 7.0 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3cccc(C(=O)O)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323081 120479 0 None -1 2 Mouse 7.0 pIC50 = 7.0 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3cccc(C(=O)O)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
145989896 173795 0 None -7 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human SSTR3 expressed in CHO-K1 cell membranesAntagonist activity at human SSTR3 expressed in CHO-K1 cell membranes
ChEMBL 517 9 1 4 7.2 CCOc1cc(CN2CCC(c3ncc(-c4ccc(F)cc4)[nH]3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4288417 173795 0 None -7 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human SSTR3 expressed in CHO-K1 cell membranesAntagonist activity at human SSTR3 expressed in CHO-K1 cell membranes
ChEMBL 517 9 1 4 7.2 CCOc1cc(CN2CCC(c3ncc(-c4ccc(F)cc4)[nH]3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
70697098 83623 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@H](C4CCOCC4)N3)n2)cc1 10.1021/ml200272z
CHEMBL2069503 83623 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@H](C4CCOCC4)N3)n2)cc1 10.1021/ml200272z
122179451 128226 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 476 3 3 2 6.4 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(c4ccccc4)(C(F)(F)F)N3)n2)cc1 10.1021/ml500514w
CHEMBL3582311 128226 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 476 3 3 2 6.4 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(c4ccccc4)(C(F)(F)F)N3)n2)cc1 10.1021/ml500514w
122179455 128230 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 398 3 3 4 4.9 c1ccc2c3c([nH]c2c1)C(C1CCCCC1)N[C@@H](c1nc(-c2cnccn2)c[nH]1)C3 10.1021/ml500514w
CHEMBL3582315 128230 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 398 3 3 4 4.9 c1ccc2c3c([nH]c2c1)C(C1CCCCC1)N[C@@H](c1nc(-c2cnccn2)c[nH]1)C3 10.1021/ml500514w
46830055 128253 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 525 5 3 9 3.2 CCn1cc(C2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582337 128253 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 525 5 3 9 3.2 CCn1cc(C2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
118710530 120477 0 None -1 2 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)nc1 10.1021/ml500028c
CHEMBL3323079 120477 0 None -1 2 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)nc1 10.1021/ml500028c
118710526 120473 0 None 1 2 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccnc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
CHEMBL3323075 120473 0 None 1 2 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccnc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
122179447 128222 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 332 2 3 2 4.1 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)CN3)n2)cc1 10.1021/ml500514w
CHEMBL3582307 128222 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 332 2 3 2 4.1 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)CN3)n2)cc1 10.1021/ml500514w
122179450 128225 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 422 3 3 2 5.8 CC1(c2ccccc2)N[C@@H](c2nc(-c3ccc(F)cc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/ml500514w
CHEMBL3582310 128225 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 422 3 3 2 5.8 CC1(c2ccccc2)N[C@@H](c2nc(-c3ccc(F)cc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/ml500514w
122179449 128224 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 397 3 2 2 6.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)O3)n2)cc1 10.1021/ml500514w
CHEMBL3582309 128224 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 397 3 2 2 6.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)O3)n2)cc1 10.1021/ml500514w
57384077 83622 0 None 1 2 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at mouse SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml200272z
CHEMBL2069502 83622 0 None 1 2 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at mouse SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml200272z
57384077 83622 0 None 1 2 Mouse 7.8 pIC50 = 7.8 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml300063m
CHEMBL2069502 83622 0 None 1 2 Mouse 7.8 pIC50 = 7.8 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml300063m
118710533 120481 0 None 3 2 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3cc(C(=O)O)ccn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323083 120481 0 None 3 2 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3cc(C(=O)O)ccn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
122179454 128229 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 397 3 3 3 5.5 c1ccc2c3c([nH]c2c1)C(C1CCCCC1)N[C@@H](c1nc(-c2ccncc2)c[nH]1)C3 10.1021/ml500514w
CHEMBL3582314 128229 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 397 3 3 3 5.5 c1ccc2c3c([nH]c2c1)C(C1CCCCC1)N[C@@H](c1nc(-c2ccncc2)c[nH]1)C3 10.1021/ml500514w
122179473 128249 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 497 4 4 8 2.7 Cn1nc([C@]2(c3cn[nH]c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)oc1=O 10.1021/ml500514w
CHEMBL3582333 128249 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 497 4 4 8 2.7 Cn1nc([C@]2(c3cn[nH]c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)oc1=O 10.1021/ml500514w
71462982 90429 0 None 1 2 Mouse 7.8 pIC50 = 7.8 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 414 3 3 5 4.4 Cc1nc([C@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204932 90429 0 None 1 2 Mouse 7.8 pIC50 = 7.8 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 414 3 3 5 4.4 Cc1nc([C@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
70688793 83633 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 454 3 4 3 4.5 CNC(=O)N1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL2069513 83633 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 454 3 4 3 4.5 CNC(=O)N1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
118710537 120485 0 None -4 2 Mouse 5.7 pIC50 = 5.7 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3ccc(C(=O)O)cn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323087 120485 0 None -4 2 Mouse 5.7 pIC50 = 5.7 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3ccc(C(=O)O)cn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
70690870 83624 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 384 3 3 3 4.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCOC4)N3)n2)cc1 10.1021/ml200272z
CHEMBL2069504 83624 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 384 3 3 3 4.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCOC4)N3)n2)cc1 10.1021/ml200272z
71462982 90429 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 414 3 3 5 4.4 Cc1nc([C@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204932 90429 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 414 3 3 5 4.4 Cc1nc([C@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
44332931 11397 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c(C3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/jm0108449
CHEMBL102892 11397 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c(C3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/jm0108449
CHEMBL1201959 11397 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c(C3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/jm0108449
137062183 128238 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 497 4 4 9 3.1 Cn1cc([C@@]2(c3noc(O)n3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582322 128238 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 497 4 4 9 3.1 Cn1cc([C@@]2(c3noc(O)n3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
122179471 128247 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 524 6 4 9 3.9 CCn1cc([C@@]2(c3nnc(NC)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582331 128247 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 524 6 4 9 3.9 CCn1cc([C@@]2(c3nnc(NC)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
118710536 120484 0 None 4 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3ccc(C(=O)O)cn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3323086 120484 0 None 4 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3ccc(C(=O)O)cn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
71452298 90431 0 None -1 2 Mouse 8.6 pIC50 = 8.6 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 484 4 3 2 6.9 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(c4ccccc4)(c4ccccc4)N3)n2)cc1 10.1021/ml300063m
CHEMBL2204934 90431 0 None -1 2 Mouse 8.6 pIC50 = 8.6 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 484 4 3 2 6.9 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(c4ccccc4)(c4ccccc4)N3)n2)cc1 10.1021/ml300063m
122179457 128232 0 None 794 4 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 495 4 3 8 3.7 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml500514w
CHEMBL3582317 128232 0 None 794 4 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 495 4 3 8 3.7 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml500514w
11112736 23301 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAntagonist activity at human SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/ml500079u
CHEMBL1237140 23301 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAntagonist activity at human SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/ml500079u
CHEMBL1788167 23301 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assayAntagonist activity at human SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/ml500079u
2070 7484 5 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/jm0108449
9802572 7484 5 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/jm0108449
CHEMBL2069499 7484 5 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/jm0108449
118710535 120483 0 None 2 2 Mouse 8.5 pIC50 = 8.5 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3cncc(C(=O)O)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323085 120483 0 None 2 2 Mouse 8.5 pIC50 = 8.5 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3cncc(C(=O)O)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
57384077 83622 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml200272z
CHEMBL2069502 83622 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml200272z
70697099 83629 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 397 3 4 3 4.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCNCC4)N3)n2)cc1 10.1021/ml200272z
CHEMBL2069509 83629 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 397 3 4 3 4.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCNCC4)N3)n2)cc1 10.1021/ml200272z
70688792 83626 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 430 3 3 3 4.6 [O-][S+]1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL2069506 83626 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 430 3 3 3 4.6 [O-][S+]1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
118710528 120475 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cncc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
CHEMBL3323077 120475 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cncc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
11069321 83620 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/ml200272z
CHEMBL2069500 83620 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/ml200272z
71457622 90428 0 None 1 2 Mouse 7.6 pIC50 = 7.6 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 412 3 3 4 4.4 Cn1cc([C@@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
CHEMBL2204931 90428 0 None 1 2 Mouse 7.6 pIC50 = 7.6 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 412 3 3 4 4.4 Cn1cc([C@@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
71452299 90437 0 None -1 2 Mouse 7.6 pIC50 = 7.6 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 416 3 3 3 5.1 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml300063m
CHEMBL2204941 90437 0 None -1 2 Mouse 7.6 pIC50 = 7.6 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 416 3 3 3 5.1 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml300063m
11069321 83620 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/ml500514w
CHEMBL2069500 83620 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/ml500514w
122179452 128227 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 397 3 3 3 5.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)nc1 10.1021/ml500514w
CHEMBL3582312 128227 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 397 3 3 3 5.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)nc1 10.1021/ml500514w
122179453 128228 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 397 3 3 3 5.5 c1cncc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)c1 10.1021/ml500514w
CHEMBL3582313 128228 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 397 3 3 3 5.5 c1cncc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)c1 10.1021/ml500514w
71452297 90430 0 None 1 2 Mouse 7.5 pIC50 = 7.5 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 414 3 3 5 4.4 Cc1nc([C@@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204933 90430 0 None 1 2 Mouse 7.5 pIC50 = 7.5 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 414 3 3 5 4.4 Cc1nc([C@@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
70684549 83627 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 446 3 3 4 4.3 O=S1(=O)CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL2069507 83627 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 446 3 3 4 4.3 O=S1(=O)CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
122179468 128244 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 527 5 4 9 4.2 CCn1cc([C@@]2(c3nnc(S)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582328 128244 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 527 5 4 9 4.2 CCn1cc([C@@]2(c3nnc(S)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
118710524 120471 0 None 1 2 Mouse 8.5 pIC50 = 8.5 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cccc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)n1 10.1021/ml500028c
CHEMBL3323073 120471 0 None 1 2 Mouse 8.5 pIC50 = 8.5 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cccc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)n1 10.1021/ml500028c
122179467 128243 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 511 5 4 9 3.6 CCn1cc([C@@]2(c3nnc(O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582327 128243 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 511 5 4 9 3.6 CCn1cc([C@@]2(c3nnc(O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
71450468 90433 0 None -1 2 Human 8.4 pIC50 = 8.4 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@@]2(c3cnn(C)c3)N[C@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204937 90433 0 None -1 2 Human 8.4 pIC50 = 8.4 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@@]2(c3cnn(C)c3)N[C@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
71454093 90432 0 None -1 2 Mouse 8.4 pIC50 = 8.4 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204936 90432 0 None -1 2 Mouse 8.4 pIC50 = 8.4 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
70690870 83624 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 384 3 3 3 4.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCOC4)N3)n2)cc1 10.1021/ml200272z
CHEMBL2069504 83624 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 384 3 3 3 4.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCOC4)N3)n2)cc1 10.1021/ml200272z
118710530 120477 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)nc1 10.1021/ml500028c
CHEMBL3323079 120477 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)nc1 10.1021/ml500028c
145953024 169369 0 None -7 5 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human SSTR3 expressed in HEK293 cells assessed as [Tyr1]-somatostatin 14-induced beta-arrestin recruitment pre-incubated for 30 mins before [Tyr1]-somatostatin 14 stimulation for 90 or 180 mins by chemiluminescence methodAntagonist activity at human SSTR3 expressed in HEK293 cells assessed as [Tyr1]-somatostatin 14-induced beta-arrestin recruitment pre-incubated for 30 mins before [Tyr1]-somatostatin 14 stimulation for 90 or 180 mins by chemiluminescence method
ChEMBL 886 20 2 10 3.4 CC[C@H](C)[C@@H](OC(=O)/C=C/c1ccccc1)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)OC 10.1021/acs.jmedchem.8b00885
CHEMBL4168948 169369 0 None -7 5 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human SSTR3 expressed in HEK293 cells assessed as [Tyr1]-somatostatin 14-induced beta-arrestin recruitment pre-incubated for 30 mins before [Tyr1]-somatostatin 14 stimulation for 90 or 180 mins by chemiluminescence methodAntagonist activity at human SSTR3 expressed in HEK293 cells assessed as [Tyr1]-somatostatin 14-induced beta-arrestin recruitment pre-incubated for 30 mins before [Tyr1]-somatostatin 14 stimulation for 90 or 180 mins by chemiluminescence method
ChEMBL 886 20 2 10 3.4 CC[C@H](C)[C@@H](OC(=O)/C=C/c1ccccc1)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)OC 10.1021/acs.jmedchem.8b00885
71457622 90428 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 412 3 3 4 4.4 Cn1cc([C@@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
CHEMBL2204931 90428 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 412 3 3 4 4.4 Cn1cc([C@@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
118710531 120478 0 None 1 2 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cccc(C(=O)O)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323080 120478 0 None 1 2 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cccc(C(=O)O)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
70688792 83626 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 430 3 3 3 4.6 [O-][S+]1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL2069506 83626 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 430 3 3 3 4.6 [O-][S+]1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
71462984 90438 0 None 1 2 Mouse 8.4 pIC50 = 8.4 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 412 3 3 4 4.4 Cn1cc([C@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
CHEMBL2204942 90438 0 None 1 2 Mouse 8.4 pIC50 = 8.4 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 412 3 3 4 4.4 Cn1cc([C@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
122179474 128250 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 511 4 3 9 2.7 Cn1cc([C@@]2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582334 128250 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 511 4 3 9 2.7 Cn1cc([C@@]2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
122179472 128248 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 538 6 3 9 3.9 CCn1cc([C@@]2(c3nnc(N(C)C)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582332 128248 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 538 6 3 9 3.9 CCn1cc([C@@]2(c3nnc(N(C)C)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
122179456 128231 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 415 3 3 3 5.6 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)nc1 10.1021/ml500514w
CHEMBL3582316 128231 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 415 3 3 3 5.6 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)nc1 10.1021/ml500514w
122179466 128242 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 509 5 3 8 4.2 CCn1cc([C@@]2(c3nnc(C)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582326 128242 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 509 5 3 8 4.2 CCn1cc([C@@]2(c3nnc(C)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
71450468 90433 0 None 1 2 Mouse 8.3 pIC50 = 8.3 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@@]2(c3cnn(C)c3)N[C@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204937 90433 0 None 1 2 Mouse 8.3 pIC50 = 8.3 Functional
Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@@]2(c3cnn(C)c3)N[C@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
11048825 115833 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.
ChEMBL 460 8 3 2 7.7 CCCCC1(CCCC)NC(c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccc(Cl)cc21 10.1021/jm0108449
CHEMBL321282 115833 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.
ChEMBL 460 8 3 2 7.7 CCCCC1(CCCC)NC(c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccc(Cl)cc21 10.1021/jm0108449
10917657 66841 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.
ChEMBL 468 10 3 2 8.1 CCCCCC1(CCCCC)NC(c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccc(C)cc21 10.1021/jm0108449
CHEMBL173778 66841 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.
ChEMBL 468 10 3 2 8.1 CCCCCC1(CCCCC)NC(c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccc(C)cc21 10.1021/jm0108449
70682467 83630 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 439 3 3 3 4.7 CC(=O)N1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL2069510 83630 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 439 3 3 3 4.7 CC(=O)N1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
118710526 120473 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccnc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
CHEMBL3323075 120473 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccnc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
122179465 128241 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 509 5 3 8 4.0 CCc1nnc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)o1 10.1021/ml500514w
CHEMBL3582325 128241 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 509 5 3 8 4.0 CCc1nnc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)o1 10.1021/ml500514w
118710529 120476 0 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)nc1 10.1021/ml500028c
CHEMBL3323078 120476 0 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)nc1 10.1021/ml500028c
122179470 128246 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 496 4 4 9 3.0 Cn1cc([C@@]2(c3nnc(N)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582330 128246 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 496 4 4 9 3.0 Cn1cc([C@@]2(c3nnc(N)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
118710524 120471 0 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cccc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)n1 10.1021/ml500028c
CHEMBL3323073 120471 0 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cccc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)n1 10.1021/ml500028c
73348312 96013 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.
ChEMBL 410 3 3 2 6.2 CC1(C2CCCCC2)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL2367844 96013 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.
ChEMBL 410 3 3 2 6.2 CC1(C2CCCCC2)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
71452299 90437 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 416 3 3 3 5.1 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml300063m
CHEMBL2204941 90437 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 416 3 3 3 5.1 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml300063m
118710533 120481 0 None -3 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3cc(C(=O)O)ccn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323083 120481 0 None -3 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3cc(C(=O)O)ccn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
122179448 128223 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 331 2 2 1 5.0 Fc1ccc(-c2c[nH]c([C@@H]3CCc4[nH]c5ccccc5c4C3)n2)cc1 10.1021/ml500514w
CHEMBL3582308 128223 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 331 2 2 1 5.0 Fc1ccc(-c2c[nH]c([C@@H]3CCc4[nH]c5ccccc5c4C3)n2)cc1 10.1021/ml500514w
118710536 120484 0 None -4 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3ccc(C(=O)O)cn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323086 120484 0 None -4 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3ccc(C(=O)O)cn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
71452297 90430 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 414 3 3 5 4.4 Cc1nc([C@@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204933 90430 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 414 3 3 5 4.4 Cc1nc([C@@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
118710535 120483 0 None -2 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3cncc(C(=O)O)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323085 120483 0 None -2 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3cncc(C(=O)O)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
11112736 23301 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL1237140 23301 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL1788167 23301 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
122179464 128240 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 495 4 3 8 3.7 Cc1nnc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)o1 10.1021/ml500514w
CHEMBL3582324 128240 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 495 4 3 8 3.7 Cc1nnc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)o1 10.1021/ml500514w
145958767 169034 0 None -1 3 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human SSTR3 expressed in HEK293 cells assessed as [Tyr1]-somatostatin 14-induced beta-arrestin recruitment pre-incubated for 30 mins before [Tyr1]-somatostatin 14 stimulation for 90 or 180 mins by chemiluminescence methodAntagonist activity at human SSTR3 expressed in HEK293 cells assessed as [Tyr1]-somatostatin 14-induced beta-arrestin recruitment pre-incubated for 30 mins before [Tyr1]-somatostatin 14 stimulation for 90 or 180 mins by chemiluminescence method
ChEMBL 932 22 2 11 2.8 CC[C@H](C)[C@@H](OC(=O)[C@H](Cc1ccccc1)N(C)C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)OC 10.1021/acs.jmedchem.8b00885
CHEMBL4163618 169034 0 None -1 3 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human SSTR3 expressed in HEK293 cells assessed as [Tyr1]-somatostatin 14-induced beta-arrestin recruitment pre-incubated for 30 mins before [Tyr1]-somatostatin 14 stimulation for 90 or 180 mins by chemiluminescence methodAntagonist activity at human SSTR3 expressed in HEK293 cells assessed as [Tyr1]-somatostatin 14-induced beta-arrestin recruitment pre-incubated for 30 mins before [Tyr1]-somatostatin 14 stimulation for 90 or 180 mins by chemiluminescence method
ChEMBL 932 22 2 11 2.8 CC[C@H](C)[C@@H](OC(=O)[C@H](Cc1ccccc1)N(C)C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)OC 10.1021/acs.jmedchem.8b00885
25204216 83632 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 455 3 3 4 5.0 COC(=O)N1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL2069512 83632 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysisAntagonist activity at human SST3 receptor expressed in CHO cells assessed as inhibition of forskolin/SS-14-stimulated cAMP accumulation preincubated for 15 mins before SS-14 challenge measured after 1 hr by time-resolved fluorescence analysis
ChEMBL 455 3 3 4 5.0 COC(=O)N1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
118710531 120478 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cccc(C(=O)O)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323080 120478 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cccc(C(=O)O)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
71452298 90431 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 484 4 3 2 6.9 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(c4ccccc4)(c4ccccc4)N3)n2)cc1 10.1021/ml300063m
CHEMBL2204934 90431 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 484 4 3 2 6.9 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(c4ccccc4)(c4ccccc4)N3)n2)cc1 10.1021/ml300063m
59411406 128254 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 525 5 3 9 3.2 CCn1cc(C2(c3nn(C)c(=O)o3)NC(c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582338 128254 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assayAntagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
ChEMBL 525 5 3 9 3.2 CCn1cc(C2(c3nn(C)c(=O)o3)NC(c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
118710528 120475 0 None 1 2 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cncc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
CHEMBL3323077 120475 0 None 1 2 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cncc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
118710536 120484 0 None 4 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3ccc(C(=O)O)cn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323086 120484 0 None 4 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysisAntagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3ccc(C(=O)O)cn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
71462984 90438 0 None -1 2 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 412 3 3 4 4.4 Cn1cc([C@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
CHEMBL2204942 90438 0 None -1 2 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 minsInhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins
ChEMBL 412 3 3 4 4.4 Cn1cc([C@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
9910573 83621 1 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human SST3 receptorAntagonist activity at human SST3 receptor
ChEMBL 430 8 3 4 4.7 CCOCC1(COCC)N[C@@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/ml200272z
CHEMBL2069501 83621 1 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human SST3 receptorAntagonist activity at human SST3 receptor
ChEMBL 430 8 3 4 4.7 CCOCC1(COCC)N[C@@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/ml200272z
154734381 224493 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
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
145705877 224515 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
2072 8994 0 None - 1 Mouse 10.1 pIC50 = 10.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2019 10447 0 None 10 4 Mouse 10.1 pIC50 = 10.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
44386062 10447 0 None 10 4 Mouse 10.1 pIC50 = 10.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
CHEMBL440072 10447 0 None 10 4 Mouse 10.1 pIC50 = 10.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
16133849 10448 12 None 8 4 Mouse 10.2 pIC50 = 10.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2020 10448 12 None 8 4 Mouse 10.2 pIC50 = 10.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
91935900 10448 12 None 8 4 Mouse 10.2 pIC50 = 10.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
CHEMBL501796 10448 12 None 8 4 Mouse 10.2 pIC50 = 10.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2068 7431 0 None - 1 Mouse 10.4 pIC50 = 10.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2036 7430 0 None 15848 2 Mouse 10.7 pIC50 = 10.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2036 7430 0 None -15848 2 Rat 6.5 pIC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9166718
2053 9623 0 None -79 3 Human 6.5 pIC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15709181
2017 9520 0 None -7079 2 Mouse 7.0 pIC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2035 7427 0 None -31622 2 Mouse 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2026 7441 0 None -1 5 Human 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11897676
2027 7442 0 None -6 5 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11897676
2042 7487 0 None -39 3 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15709181
2041 7437 0 None -125 3 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9045884
2032 7424 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2051 10349 24 None -7 4 Mouse 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
5311430 10349 24 None -7 4 Mouse 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
CHEMBL311695 10349 24 None -7 4 Mouse 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2037 7432 0 None -794 2 Mouse 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2031 9053 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
71349 9053 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
DB06791 9053 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2003 7428 0 None 79 2 Mouse 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2012 8157 0 None -3 4 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15658864
2055 9682 48 None -8 5 Mouse 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
383414 9682 48 None -8 5 Mouse 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
90488715 9682 48 None -8 5 Mouse 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
CHEMBL1680 9682 48 None -8 5 Mouse 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
CHEMBL262746 9682 48 None -8 5 Mouse 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
DB00104 9682 48 None -8 5 Mouse 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2013 8961 0 None -2 6 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12450568
2018 9781 28 None -10 5 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15477717
9941444 9781 28 None -10 5 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15477717
CHEMBL3349607 9781 28 None -10 5 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15477717
DB06663 9781 28 None -10 5 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15477717
2039 7434 0 None 3 2 Mouse 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2040 7435 0 None -5 2 Mouse 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
10114 9334 23 None -1 6 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 494 4 3 7 4.3 Fc1ccc(cc1)c1cnc([nH]1)[C@H]1Cc2c3ccccc3[nH]c2[C@@](N1)(c1noc(n1)C)c1cnn(c1)C 24900499
56927659 9334 23 None -1 6 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 494 4 3 7 4.3 Fc1ccc(cc1)c1cnc([nH]1)[C@H]1Cc2c3ccccc3[nH]c2[C@@](N1)(c1noc(n1)C)c1cnn(c1)C 24900499
CHEMBL2204935 9334 23 None -1 6 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 494 4 3 7 4.3 Fc1ccc(cc1)c1cnc([nH]1)[C@H]1Cc2c3ccccc3[nH]c2[C@@](N1)(c1noc(n1)C)c1cnn(c1)C 24900499
2004 7429 0 None 19 2 Mouse 9.4 pIC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2077 10453 0 None - 1 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11095748




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DOI

162648021 186752 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at SST3 (unknown origin)Agonist activity at SST3 (unknown origin)
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(F)c4O)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4746816 186752 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at SST3 (unknown origin)Agonist activity at SST3 (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
140762500 188512 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at SST3 (unknown origin)Agonist activity at SST3 (unknown origin)
ChEMBL 529 5 1 5 6.1 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)cc(C#N)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4777122 188512 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at SST3 (unknown origin)Agonist activity at SST3 (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
CHEMBL5276605 200685 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human SST3 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST3 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 474 3 2 5 5.5 N#Cc1cc(F)cc(-c2ccc3ncc(-c4cc(F)cc(F)c4)c(N4CCC(N)CC4)c3c2)c1O 10.1021/acsmedchemlett.2c00431
140762573 189156 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at SST3 (unknown origin)Agonist activity at SST3 (unknown origin)
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(O)ccc4F)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4785112 189156 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at SST3 (unknown origin)Agonist activity at SST3 (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
140762567 187056 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at SST3 (unknown origin)Agonist activity at SST3 (unknown origin)
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(O)cc(F)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4750691 187056 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at SST3 (unknown origin)Agonist activity at SST3 (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 188043 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at SST3 (unknown origin)Agonist activity at SST3 (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 188043 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at SST3 (unknown origin)Agonist activity at SST3 (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
124168080 188613 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human SST3Agonist activity at human SST3
ChEMBL 507 6 2 7 4.4 Cc1cc(Cl)cc(-c2cnc3ncn(-c4cc(O)cc(F)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4778342 188613 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human SST3Agonist activity at human SST3
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
16129706 215810 40 None - 5 Mouse 10.1 pIC50 = 10.1 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm960850i
CHEMBL1823872 215810 40 None - 5 Mouse 10.1 pIC50 = 10.1 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3
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
10114 9334 23 None - 0 Mouse 9.4 pIC50 = 9.4 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Fc1ccc(cc1)c1cnc([nH]1)[C@H]1Cc2c3ccccc3[nH]c2[C@@](N1)(c1noc(n1)C)c1cnn(c1)C 10.1021/ml300063m
56927659 9334 23 None - 0 Mouse 9.4 pIC50 = 9.4 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Fc1ccc(cc1)c1cnc([nH]1)[C@H]1Cc2c3ccccc3[nH]c2[C@@](N1)(c1noc(n1)C)c1cnn(c1)C 10.1021/ml300063m
CHEMBL2204935 9334 23 None - 0 Mouse 9.4 pIC50 = 9.4 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 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
16129706 215810 40 None -4 5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration against human somatostatin receptor type 3 in CHO-K1 cellsInhibitory concentration against human somatostatin receptor type 3 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/jm050376t
CHEMBL1823872 215810 40 None -4 5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration against human somatostatin receptor type 3 in CHO-K1 cellsInhibitory concentration against human somatostatin receptor type 3 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/jm050376t
118710523 120470 0 None - 0 Mouse 9.4 pIC50 = 9.4 Binding
Displacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cccc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)n1 10.1021/ml500028c
CHEMBL3323072 120470 0 None - 0 Mouse 9.4 pIC50 = 9.4 Binding
Displacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cccc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)n1 10.1021/ml500028c
118710525 120472 0 None - 0 Mouse 9.4 pIC50 = 9.4 Binding
Displacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccnc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
CHEMBL3323074 120472 0 None - 0 Mouse 9.4 pIC50 = 9.4 Binding
Displacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccnc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
71459516 90435 0 None - 0 Mouse 9.3 pIC50 = 9.3 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 492 4 3 6 4.3 Cn1cc(C2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
CHEMBL2204939 90435 0 None - 0 Mouse 9.3 pIC50 = 9.3 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 492 4 3 6 4.3 Cn1cc(C2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
71462983 90434 0 None - 0 Mouse 9.3 pIC50 = 9.3 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@]2(c3cnn(C)c3)N[C@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204938 90434 0 None - 0 Mouse 9.3 pIC50 = 9.3 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@]2(c3cnn(C)c3)N[C@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
71461260 90436 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 496 4 3 8 4.3 Cc1nc(C2(c3noc(C)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204940 90436 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 496 4 3 8 4.3 Cc1nc(C2(c3noc(C)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
122179477 128252 5 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity to rat SSTR3Binding affinity to rat SSTR3
ChEMBL 525 5 3 9 3.2 CCn1cc([C@@]2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582336 128252 5 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity to rat SSTR3Binding affinity to rat SSTR3
ChEMBL 525 5 3 9 3.2 CCn1cc([C@@]2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
71454093 90432 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204936 90432 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
118710525 120472 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccnc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
CHEMBL3323074 120472 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccnc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
10114 9334 23 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
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 10.1016/j.bmcl.2016.02.022
56927659 9334 23 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
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 10.1016/j.bmcl.2016.02.022
CHEMBL2204935 9334 23 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
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 10.1016/j.bmcl.2016.02.022
10114 9334 23 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Fc1ccc(cc1)c1cnc([nH]1)[C@H]1Cc2c3ccccc3[nH]c2[C@@](N1)(c1noc(n1)C)c1cnn(c1)C 10.1021/ml300063m
56927659 9334 23 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Fc1ccc(cc1)c1cnc([nH]1)[C@H]1Cc2c3ccccc3[nH]c2[C@@](N1)(c1noc(n1)C)c1cnn(c1)C 10.1021/ml300063m
CHEMBL2204935 9334 23 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 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
10114 9334 23 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
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/ml500514w
56927659 9334 23 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
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/ml500514w
CHEMBL2204935 9334 23 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
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/ml500514w
118710524 120471 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Displacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cccc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)n1 10.1021/ml500028c
CHEMBL3323073 120471 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Displacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cccc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)n1 10.1021/ml500028c
71459516 90435 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 492 4 3 6 4.3 Cn1cc(C2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
CHEMBL2204939 90435 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 492 4 3 6 4.3 Cn1cc(C2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
71452298 90431 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 484 4 3 2 6.9 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(c4ccccc4)(c4ccccc4)N3)n2)cc1 10.1021/ml300063m
CHEMBL2204934 90431 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 484 4 3 2 6.9 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(c4ccccc4)(c4ccccc4)N3)n2)cc1 10.1021/ml300063m
118710527 120474 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cncc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
CHEMBL3323076 120474 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cncc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
11069321 83620 0 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/ml200272z
CHEMBL2069500 83620 0 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/ml200272z
11069321 83620 0 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/ml500514w
CHEMBL2069500 83620 0 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/ml500514w
118710523 120470 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cccc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)n1 10.1021/ml500028c
CHEMBL3323072 120470 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cccc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)n1 10.1021/ml500028c
71462983 90434 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@]2(c3cnn(C)c3)N[C@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204938 90434 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@]2(c3cnn(C)c3)N[C@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
71461260 90436 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 496 4 3 8 4.3 Cc1nc(C2(c3noc(C)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204940 90436 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 496 4 3 8 4.3 Cc1nc(C2(c3noc(C)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL1824052 215815 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst3 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
CHEMBL442494 220692 0 None -4 5 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to human sst3 by in vitro receptor autoradiography assayBinding affinity to human sst3 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
122179461 128237 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 535 6 3 8 4.6 Cc1nc([C@]2(c3cnn(CC4CC4)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml500514w
CHEMBL3582321 128237 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 535 6 3 8 4.6 Cc1nc([C@]2(c3cnn(CC4CC4)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml500514w
71454093 90432 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204936 90432 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
86766278 137338 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.
ChEMBL 539 5 3 7 4.9 COC1CC2C(C1)C2C1(c2nnc(C)o2)N[C@@H](c2nc(-c3ccc(F)c(C)n3)c[nH]2)Cc2c1[nH]c1ccccc21 nan
CHEMBL3680938 137338 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.
ChEMBL 539 5 3 7 4.9 COC1CC2C(C1)C2C1(c2nnc(C)o2)N[C@@H](c2nc(-c3ccc(F)c(C)n3)c[nH]2)Cc2c1[nH]c1ccccc21 nan
71450468 90433 0 None - 0 Mouse 8.9 pIC50 = 8.9 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@@]2(c3cnn(C)c3)N[C@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204937 90433 0 None - 0 Mouse 8.9 pIC50 = 8.9 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@@]2(c3cnn(C)c3)N[C@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
118710534 120482 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cncc(C(=O)O)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323084 120482 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cncc(C(=O)O)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
122179477 128252 5 None - 0 Mouse 8.9 pIC50 = 8.9 Binding
Displacement of [125I]SS-14 from mouse recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from mouse recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 525 5 3 9 3.2 CCn1cc([C@@]2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582336 128252 5 None - 0 Mouse 8.9 pIC50 = 8.9 Binding
Displacement of [125I]SS-14 from mouse recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from mouse recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 525 5 3 9 3.2 CCn1cc([C@@]2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
127030549 145300 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 476 4 3 7 4.2 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL3775042 145300 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 476 4 3 7 4.2 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
122179480 128258 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 565 7 3 9 4.0 CCn1cc([C@@]2(c3nn(CC4CC4)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582341 128258 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 565 7 3 9 4.0 CCn1cc([C@@]2(c3nn(CC4CC4)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL1824051 215814 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst3 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
118710524 120471 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cccc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)n1 10.1021/ml500028c
CHEMBL3323073 120471 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cccc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)n1 10.1021/ml500028c
68306121 137337 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.
ChEMBL 513 4 3 7 4.8 Cc1nnc(C2(C3CCCCO3)N[C@@H](c3nc(-c4ccc(F)c(C)n4)c[nH]3)Cc3c2[nH]c2ccccc32)o1 nan
CHEMBL3680937 137337 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.
ChEMBL 513 4 3 7 4.8 Cc1nnc(C2(C3CCCCO3)N[C@@H](c3nc(-c4ccc(F)c(C)n4)c[nH]3)Cc3c2[nH]c2ccccc32)o1 nan
CHEMBL442494 220692 0 None -4 5 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 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
70688791 83625 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 414 3 3 3 5.6 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCSCC4)N3)n2)cc1 10.1021/ml200272z
CHEMBL2069505 83625 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 414 3 3 3 5.6 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCSCC4)N3)n2)cc1 10.1021/ml200272z
71452299 90437 0 None - 0 Mouse 8.8 pIC50 = 8.8 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 416 3 3 3 5.1 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml300063m
CHEMBL2204941 90437 0 None - 0 Mouse 8.8 pIC50 = 8.8 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 416 3 3 3 5.1 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml300063m
118710529 120476 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)nc1 10.1021/ml500028c
CHEMBL3323078 120476 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)nc1 10.1021/ml500028c
86279005 120480 2 None - 0 Mouse 8.8 pIC50 = 8.8 Binding
Displacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cc(C(=O)O)ccn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323082 120480 2 None - 0 Mouse 8.8 pIC50 = 8.8 Binding
Displacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cc(C(=O)O)ccn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
127030230 145361 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 434 3 3 3 5.2 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1F 10.1016/j.bmcl.2016.02.022
CHEMBL3775532 145361 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 434 3 3 3 5.2 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1F 10.1016/j.bmcl.2016.02.022
122179469 128245 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 541 6 3 9 4.6 CCn1cc([C@@]2(c3nnc(SC)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582329 128245 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 541 6 3 9 4.6 CCn1cc([C@@]2(c3nnc(SC)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
127032662 145333 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 454 3 3 4 6.1 c1ccc2c3c([nH]c2c1)[C@@H](C1CCOCC1)N[C@@H](c1nc(-c2csc4ccccc24)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
CHEMBL3775284 145333 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 454 3 3 4 6.1 c1ccc2c3c([nH]c2c1)[C@@H](C1CCOCC1)N[C@@H](c1nc(-c2csc4ccccc24)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
CHEMBL3350912 218309 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
118710535 120483 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3cncc(C(=O)O)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323085 120483 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3cncc(C(=O)O)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL2079558 215973 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
CHEMBL2079626 215976 2 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
CHEMBL3349611 218217 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
49865345 22683 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST3 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST3 receptor expressed in human CCL39 cells by autoradiography
ChEMBL 1043 18 13 12 0.7 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C/C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cc3ccccc3[nH]2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1 10.1021/jm1005868
CHEMBL1223230 22683 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST3 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST3 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
CHEMBL2372606 217055 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccccc2)NC[C@H]2O[C@H](O)[C@H](O)[C@@H](O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL2372608 217055 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 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
127034125 145390 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 412 3 3 3 5.1 CC1(c2nc(-c3ccccc3)c[nH]2)Cc2c([nH]c3ccccc23)C(C2CCOCC2)N1 10.1016/j.bmcl.2016.02.022
CHEMBL3775729 145390 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 412 3 3 3 5.1 CC1(c2nc(-c3ccccc3)c[nH]2)Cc2c([nH]c3ccccc23)C(C2CCOCC2)N1 10.1016/j.bmcl.2016.02.022
44560867 195919 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiography
ChEMBL 1204 18 12 14 1.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N(C)C(=O)c2ccccc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL510693 195919 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
CHEMBL3350725 218269 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)c(I)c2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030245x
CHEMBL425465 220114 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL None None None CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)O)CSSC[C@@H](N)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049520l
2051 10349 24 None -218 9 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human sst3 by in vitro receptor autoradiography assayBinding affinity to human sst3 by in vitro receptor autoradiography assay
ChEMBL None None None None 10.1021/ml200032v
5311430 10349 24 None -218 9 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human sst3 by in vitro receptor autoradiography assayBinding affinity to human sst3 by in vitro receptor autoradiography assay
ChEMBL None None None None 10.1021/ml200032v
CHEMBL311695 10349 24 None -218 9 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human sst3 by in vitro receptor autoradiography assayBinding affinity to human sst3 by in vitro receptor autoradiography assay
ChEMBL None None None None 10.1021/ml200032v
25189327 19468 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 601 11 4 4 4.7 NCCCC[C@@H](C(=O)NCc1cccc2ccccc12)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1187509 19468 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 601 11 4 4 4.7 NCCCC[C@@H](C(=O)NCc1cccc2ccccc12)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL505888 19468 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 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
CHEMBL3351090 218323 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
127033551 145351 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 399 3 3 4 4.3 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)nc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775418 145351 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 399 3 3 4 4.3 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)nc1 10.1016/j.bmcl.2016.02.022
CHEMBL410047 219576 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3
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
122179452 128227 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 397 3 3 3 5.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)nc1 10.1021/ml500514w
CHEMBL3582312 128227 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 397 3 3 3 5.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)nc1 10.1021/ml500514w
122179447 128222 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 332 2 3 2 4.1 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)CN3)n2)cc1 10.1021/ml500514w
CHEMBL3582307 128222 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 332 2 3 2 4.1 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)CN3)n2)cc1 10.1021/ml500514w
122179454 128229 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 397 3 3 3 5.5 c1ccc2c3c([nH]c2c1)C(C1CCCCC1)N[C@@H](c1nc(-c2ccncc2)c[nH]1)C3 10.1021/ml500514w
CHEMBL3582314 128229 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 397 3 3 3 5.5 c1ccc2c3c([nH]c2c1)C(C1CCCCC1)N[C@@H](c1nc(-c2ccncc2)c[nH]1)C3 10.1021/ml500514w
CHEMBL2371059 216785 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
CHEMBL452074 220753 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst3 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst3 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
70689723 80743 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1170 16 9 12 4.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL2021559 80743 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1170 16 9 12 4.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
45273129 202516 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1173 19 14 15 1.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(C(N)=O)cc2)CSS[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)O)NC1=O 10.1021/jm801314f
CHEMBL557288 202516 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1173 19 14 15 1.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(C(N)=O)cc2)CSS[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)O)NC1=O 10.1021/jm801314f
CHEMBL510755 222367 0 None -3 3 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
CHEMBL3349506 218190 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
CHEMBL3350908 218306 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
25187685 19242 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 648 11 4 5 3.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)C2CCN(C(=O)c3ccccc3)CC2)C1=O 10.1021/jm801205x
CHEMBL1186206 19242 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 648 11 4 5 3.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)C2CCN(C(=O)c3ccccc3)CC2)C1=O 10.1021/jm801205x
CHEMBL454202 19242 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 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
CHEMBL3349666 218229 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
CHEMBL415585 219972 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 3 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
CHEMBL503596 220949 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
70684549 83627 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 446 3 3 4 4.3 O=S1(=O)CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL2069507 83627 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 446 3 3 4 4.3 O=S1(=O)CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL505704 220975 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
118718507 122136 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (hsst) receptor
ChEMBL 1050 14 11 12 3.4 CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)NC(C)(C)C)NC1=O 10.1021/jm970730q
CHEMBL3349670 122136 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
44560872 195194 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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 195194 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
44325273 214087 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration required for somatostatin 3 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 3 receptor in radioligand binding assay ([125I]Tyr11-SRIF)
ChEMBL 554 7 2 4 5.4 NCCCC1CCCN2C(=O)[C@@H](Cc3c[nH]c4ccccc34)SCCN(Cc3cccc4ccccc34)C(=O)C12 10.1016/s0960-894x(00)00552-7
CHEMBL93351 214087 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration required for somatostatin 3 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 3 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
127030228 145332 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 428 4 3 4 4.9 COc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775282 145332 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 428 4 3 4 4.9 COc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL406816 219402 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 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
CHEMBL425090 220108 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1824055 215818 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 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 220755 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030246p
CHEMBL1824055 215818 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL452157 220755 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
CHEMBL1824049 215812 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst3 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
CHEMBL1824055 215818 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm200307v
CHEMBL452157 220755 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm200307v
CHEMBL452157 220755 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL452157 220755 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm801314f
CHEMBL452157 220755 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3
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
CHEMBL265912 217450 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 3.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 3.
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+
122179463 128239 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 510 5 4 9 2.8 Cn1cc([C@@]2(c3noc(CN)n3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582323 128239 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 510 5 4 9 2.8 Cn1cc([C@@]2(c3noc(CN)n3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3349663 218226 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
CHEMBL1824053 215816 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst3 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
45102042 23803 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]iodotyrosyl from human SST3 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST3 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 23803 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]iodotyrosyl from human SST3 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST3 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
127032663 145382 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 437 3 4 3 5.4 c1ccc2c(-c3c[nH]c([C@H]4Cc5c([nH]c6ccccc56)[C@@H](C5CCOCC5)N4)n3)c[nH]c2c1 10.1016/j.bmcl.2016.02.022
CHEMBL3775643 145382 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 437 3 4 3 5.4 c1ccc2c(-c3c[nH]c([C@H]4Cc5c([nH]c6ccccc56)[C@@H](C5CCOCC5)N4)n3)c[nH]c2c1 10.1016/j.bmcl.2016.02.022
127033869 145258 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 430 3 2 4 5.1 Cn1cc(-c2ccc(F)cc2)nc1[C@H]1Cc2c([nH]c3ccccc23)[C@H](C2CCOCC2)N1 10.1016/j.bmcl.2016.02.022
CHEMBL3774771 145258 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 430 3 2 4 5.1 Cn1cc(-c2ccc(F)cc2)nc1[C@H]1Cc2c([nH]c3ccccc23)[C@H](C2CCOCC2)N1 10.1016/j.bmcl.2016.02.022
CHEMBL3350894 218295 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
118718854 122194 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350354 122194 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 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
CHEMBL3349618 218223 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
CHEMBL509363 222213 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
CHEMBL3349617 218222 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
CHEMBL415582 219969 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 3 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
57384077 83622 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL2069502 83622 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL2371100 216791 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 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
CHEMBL525030 222410 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
57384077 83622 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml200272z
CHEMBL2069502 83622 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml200272z
57384077 83622 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml300063m
CHEMBL2069502 83622 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml300063m
CHEMBL3349613 218219 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
127031455 145272 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 423 3 3 4 4.8 N#Cc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3774861 145272 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 423 3 3 4 4.8 N#Cc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3349679 218241 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
127032659 145244 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 404 3 3 4 5.0 c1ccc2c3c([nH]c2c1)[C@@H](C1CCOCC1)N[C@@H](c1nc(-c2ccsc2)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
CHEMBL3774626 145244 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 404 3 3 4 5.0 c1ccc2c3c([nH]c2c1)[C@@H](C1CCOCC1)N[C@@H](c1nc(-c2ccsc2)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
CHEMBL1824054 215817 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst3 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
CHEMBL505854 220977 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
44290766 164735 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity of human Somatostatin receptor type 3 (hsst3) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 3 (hsst3) 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 164735 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity of human Somatostatin receptor type 3 (hsst3) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 3 (hsst3) 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
127032341 145404 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 378 2 3 3 4.5 CC(C)(C)c1c[nH]c(C2Cc3c([nH]c4ccccc34)C(C3CCOCC3)N2)n1 10.1016/j.bmcl.2016.02.022
CHEMBL3775825 145404 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 378 2 3 3 4.5 CC(C)(C)c1c[nH]c(C2Cc3c([nH]c4ccccc34)C(C3CCOCC3)N2)n1 10.1016/j.bmcl.2016.02.022
CHEMBL552013 222500 3 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](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/jm801314f
25187398 19220 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 12 4 4 4.0 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1186066 19220 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 12 4 4 4.0 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL448026 19220 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 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
CHEMBL502219 220930 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
CHEMBL499760 220880 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
42637503 202596 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1238 19 12 15 2.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL558161 202596 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1238 19 12 15 2.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
11468916 122241 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1137 15 14 14 0.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
CHEMBL3350910 122241 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
CHEMBL3122123 217881 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[LTT]-SS28 from human SST3 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST3 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
CHEMBL3122127 217884 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[LTT]-SS28 from human SST3 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST3 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
70682467 83630 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 439 3 3 3 4.7 CC(=O)N1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL2069510 83630 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 439 3 3 3 4.7 CC(=O)N1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL3349680 218242 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
CHEMBL2311181 216286 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
25187679 19443 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 571 10 4 4 4.3 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccc(Cl)cc2)C1=O 10.1021/jm801205x
CHEMBL1187340 19443 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 571 10 4 4 4.3 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccc(Cl)cc2)C1=O 10.1021/jm801205x
CHEMBL499398 19443 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 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
CHEMBL1908984 215851 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](N)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC2=O)cc1 10.1021/jm801314f
CHEMBL563124 215851 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](N)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC2=O)cc1 10.1021/jm801314f
44560876 195555 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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 195555 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
127031464 145279 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 399 3 3 4 4.3 c1ccc2c3c([nH]c2c1)[C@@H](C1CCOCC1)N[C@@H](c1nc(-c2ccncc2)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
CHEMBL3774903 145279 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 399 3 3 4 4.3 c1ccc2c3c([nH]c2c1)[C@@H](C1CCOCC1)N[C@@H](c1nc(-c2ccncc2)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
CHEMBL1824057 215820 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2cn(Cc3ccccc3)cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm200307v
127032660 145353 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 438 3 3 4 5.6 Clc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)s1 10.1016/j.bmcl.2016.02.022
CHEMBL3775435 145353 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 438 3 3 4 5.6 Clc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)s1 10.1016/j.bmcl.2016.02.022
45273131 201565 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1271 20 11 14 2.8 CN(C(=O)c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(C(N)=O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm801314f
CHEMBL538451 201565 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 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
122179473 128249 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 497 4 4 8 2.7 Cn1nc([C@]2(c3cn[nH]c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)oc1=O 10.1021/ml500514w
CHEMBL3582333 128249 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 497 4 4 8 2.7 Cn1nc([C@]2(c3cn[nH]c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)oc1=O 10.1021/ml500514w
CHEMBL415359 219964 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 3 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
CHEMBL3349677 218239 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
CHEMBL2011465 215892 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human sst3 by in vitro receptor autoradiography assayBinding affinity to human sst3 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
CHEMBL2011466 215893 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human sst3 by in vitro receptor autoradiography assayBinding affinity to human sst3 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
CHEMBL3349668 218231 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
CHEMBL3349664 218227 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
CHEMBL2111257 215995 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 3 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
127031155 145226 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 416 3 3 3 5.1 Fc1ccccc1-c1c[nH]c([C@H]2Cc3c([nH]c4ccccc34)[C@@H](C3CCOCC3)N2)n1 10.1016/j.bmcl.2016.02.022
CHEMBL3774495 145226 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 416 3 3 3 5.1 Fc1ccccc1-c1c[nH]c([C@H]2Cc3c([nH]c4ccccc34)[C@@H](C3CCOCC3)N2)n1 10.1016/j.bmcl.2016.02.022
CHEMBL3350357 218254 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 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
CHEMBL3122128 217885 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[LTT]-SS28 from human SST3 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST3 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
CHEMBL502777 220936 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
25187400 19466 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 537 10 4 4 3.7 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1187495 19466 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 537 10 4 4 3.7 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL504930 19466 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 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
CHEMBL263306 217345 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 3 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
CHEMBL2372604 217054 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=5)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=5)
ChEMBL None None None C[C@H](O)[C@@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
CHEMBL2372607 217054 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=5)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 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
CHEMBL2372604 217054 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)
ChEMBL None None None C[C@H](O)[C@@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
CHEMBL2372607 217054 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 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
CHEMBL263587 217357 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3
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
CHEMBL446380 220724 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
CHEMBL447989 220732 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
71462982 90429 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 414 3 3 5 4.4 Cc1nc([C@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204932 90429 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 414 3 3 5 4.4 Cc1nc([C@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
127031465 145270 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 399 3 3 4 4.3 c1cncc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
CHEMBL3774851 145270 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 399 3 3 4 4.3 c1cncc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
CHEMBL3350887 218289 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
CHEMBL1824050 215813 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst3 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
122179476 128251 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 539 5 3 9 3.7 CC(C)n1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)oc1=O 10.1021/ml500514w
CHEMBL3582335 128251 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 539 5 3 9 3.7 CC(C)n1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)oc1=O 10.1021/ml500514w
127034429 145251 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 507 5 3 9 3.6 COc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@](c4cnn(C)c4)(c4noc(C)n4)N3)n2)n1 10.1016/j.bmcl.2016.02.022
CHEMBL3774684 145251 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 507 5 3 9 3.6 COc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@](c4cnn(C)c4)(c4noc(C)n4)N3)n2)n1 10.1016/j.bmcl.2016.02.022
122179451 128226 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 476 3 3 2 6.4 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(c4ccccc4)(C(F)(F)F)N3)n2)cc1 10.1021/ml500514w
CHEMBL3582311 128226 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 476 3 3 2 6.4 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(c4ccccc4)(C(F)(F)F)N3)n2)cc1 10.1021/ml500514w
122179479 128257 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 553 6 3 9 4.2 CCn1cc([C@@]2(c3nn(C(C)C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582340 128257 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 553 6 3 9 4.2 CCn1cc([C@@]2(c3nn(C(C)C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
122179481 128259 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 582 8 3 10 3.2 CCn1cc([C@@]2(c3nn(CCN(C)C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582342 128259 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 582 8 3 10 3.2 CCn1cc([C@@]2(c3nn(CCN(C)C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
86279005 120480 2 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cc(C(=O)O)ccn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323082 120480 2 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cc(C(=O)O)ccn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
122179459 128234 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 509 5 3 8 4.2 CCn1cc([C@@]2(c3noc(C)n3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582319 128234 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 509 5 3 8 4.2 CCn1cc([C@@]2(c3noc(C)n3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
122179466 128242 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 509 5 3 8 4.2 CCn1cc([C@@]2(c3nnc(C)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582326 128242 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 509 5 3 8 4.2 CCn1cc([C@@]2(c3nnc(C)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
122179477 128252 5 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 525 5 3 9 3.2 CCn1cc([C@@]2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582336 128252 5 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 525 5 3 9 3.2 CCn1cc([C@@]2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
71450468 90433 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@@]2(c3cnn(C)c3)N[C@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204937 90433 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 494 4 3 7 4.3 Cc1nc([C@@]2(c3cnn(C)c3)N[C@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL1823873 215811 9 None -1 4 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst3 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
CHEMBL3122130 217887 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[LTT]-SS28 from human SST3 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST3 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
122179483 128261 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 568 7 4 10 2.1 CCn1cc([C@@]2(c3nn(CC(N)=O)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582344 128261 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 568 7 4 10 2.1 CCn1cc([C@@]2(c3nn(CC(N)=O)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
122179477 128252 5 None - 0 Dog 8.6 pIC50 = 8.6 Binding
Binding affinity to dog SSTR3Binding affinity to dog SSTR3
ChEMBL 525 5 3 9 3.2 CCn1cc([C@@]2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582336 128252 5 None - 0 Dog 8.6 pIC50 = 8.6 Binding
Binding affinity to dog SSTR3Binding affinity to dog SSTR3
ChEMBL 525 5 3 9 3.2 CCn1cc([C@@]2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
68306177 137335 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.
ChEMBL 473 6 3 7 4.0 CCOC[C@@]1(c2nnc(C)o2)N[C@@H](c2nc(-c3ccc(F)cn3)c[nH]2)Cc2c1[nH]c1ccccc21 nan
CHEMBL3680935 137335 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.
ChEMBL 473 6 3 7 4.0 CCOC[C@@]1(c2nnc(C)o2)N[C@@H](c2nc(-c3ccc(F)cn3)c[nH]2)Cc2c1[nH]c1ccccc21 nan
127030550 145379 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 476 4 3 7 4.2 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL3775630 145379 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 476 4 3 7 4.2 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
122179456 128231 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 415 3 3 3 5.6 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)nc1 10.1021/ml500514w
CHEMBL3582316 128231 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 415 3 3 3 5.6 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)nc1 10.1021/ml500514w
CHEMBL442494 220692 0 None -4 5 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst3 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst3 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
71452299 90437 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 416 3 3 3 5.1 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL2204941 90437 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 416 3 3 3 5.1 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
71452299 90437 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 416 3 3 3 5.1 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml300063m
CHEMBL2204941 90437 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 416 3 3 3 5.1 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml300063m
127033002 145315 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 507 5 3 9 3.6 COc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@](c4cnn(C)c4)(c4noc(C)n4)N3)n2)n1 10.1016/j.bmcl.2016.02.022
CHEMBL3775160 145315 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 507 5 3 9 3.6 COc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@](c4cnn(C)c4)(c4noc(C)n4)N3)n2)n1 10.1016/j.bmcl.2016.02.022
122179475 128085 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 525 5 3 9 3.2 CCn1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)oc1=O 10.1021/ml500514w
CHEMBL3580681 128085 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 525 5 3 9 3.2 CCn1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)oc1=O 10.1021/ml500514w
122179460 128236 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 509 5 3 8 4.0 CCc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml500514w
CHEMBL3582320 128236 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 509 5 3 8 4.0 CCc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml500514w
118710530 120477 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)nc1 10.1021/ml500028c
CHEMBL3323079 120477 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)nc1 10.1021/ml500028c
CHEMBL504395 220955 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
122179453 128228 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 397 3 3 3 5.5 c1cncc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)c1 10.1021/ml500514w
CHEMBL3582313 128228 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 397 3 3 3 5.5 c1cncc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)c1 10.1021/ml500514w
122179458 128233 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 481 4 4 7 3.7 Cc1nc([C@]2(c3cn[nH]c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml500514w
CHEMBL3582318 128233 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 481 4 4 7 3.7 Cc1nc([C@]2(c3cn[nH]c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml500514w
CHEMBL2011467 215894 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human sst3 by in vitro receptor autoradiography assayBinding affinity to human sst3 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
CHEMBL2011462 215889 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human sst3 by in vitro receptor autoradiography assayBinding affinity to human sst3 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
70688792 83626 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 430 3 3 3 4.6 [O-][S+]1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL2069506 83626 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 430 3 3 3 4.6 [O-][S+]1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL3350891 218293 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
90663872 113515 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 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 113515 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 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 113515 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 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
CHEMBL219201 216188 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst3Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst3
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
CHEMBL3349597 218205 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
CHEMBL3350898 218299 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
70688792 83626 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 430 3 3 3 4.6 [O-][S+]1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL2069506 83626 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 430 3 3 3 4.6 [O-][S+]1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL436962 220479 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3
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
127030232 145423 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 430 3 2 4 5.1 Cn1cc(-c2ccc(F)cc2)nc1[C@H]1Cc2c([nH]c3ccccc23)[C@@H](C2CCOCC2)N1 10.1016/j.bmcl.2016.02.022
CHEMBL3775986 145423 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 430 3 2 4 5.1 Cn1cc(-c2ccc(F)cc2)nc1[C@H]1Cc2c([nH]c3ccccc23)[C@@H](C2CCOCC2)N1 10.1016/j.bmcl.2016.02.022
CHEMBL3349673 218235 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
127030231 145301 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 434 3 3 3 5.2 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c(F)c1 10.1016/j.bmcl.2016.02.022
CHEMBL3775050 145301 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 434 3 3 3 5.2 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c(F)c1 10.1016/j.bmcl.2016.02.022
127034125 145390 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 412 3 3 3 5.1 CC1(c2nc(-c3ccccc3)c[nH]2)Cc2c([nH]c3ccccc23)C(C2CCOCC2)N1 10.1016/j.bmcl.2016.02.022
CHEMBL3775729 145390 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 412 3 3 3 5.1 CC1(c2nc(-c3ccccc3)c[nH]2)Cc2c([nH]c3ccccc23)C(C2CCOCC2)N1 10.1016/j.bmcl.2016.02.022
118710536 120484 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3ccc(C(=O)O)cn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323086 120484 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3ccc(C(=O)O)cn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
127032340 145369 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 404 3 3 3 5.3 c1ccc2c3c([nH]c2c1)C(C1CCOCC1)NC(c1nc(C2CCCCC2)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
CHEMBL3775580 145369 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 404 3 3 3 5.3 c1ccc2c3c([nH]c2c1)C(C1CCOCC1)NC(c1nc(C2CCCCC2)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
45273130 202348 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 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 202348 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 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
CHEMBL3349669 218232 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
70689221 84631 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1033 12 13 14 -0.7 C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)N(C)[C@@H](O)NC1=O 10.1021/jm030243c
CHEMBL2093026 84631 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 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
127034427 145264 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 477 4 3 8 3.6 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccccn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL3774800 145264 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 477 4 3 8 3.6 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccccn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL3122129 217886 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[LTT]-SS28 from human SST3 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST3 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
46830055 128253 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 525 5 3 9 3.2 CCn1cc(C2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582337 128253 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 525 5 3 9 3.2 CCn1cc(C2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
122179448 128223 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 331 2 2 1 5.0 Fc1ccc(-c2c[nH]c([C@@H]3CCc4[nH]c5ccccc5c4C3)n2)cc1 10.1021/ml500514w
CHEMBL3582308 128223 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 331 2 2 1 5.0 Fc1ccc(-c2c[nH]c([C@@H]3CCc4[nH]c5ccccc5c4C3)n2)cc1 10.1021/ml500514w
90663868 113513 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 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 113513 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 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 113513 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 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
CHEMBL3350905 218303 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
127032342 145411 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 456 3 3 3 5.7 c1ccc2c3c([nH]c2c1)C(C1CCOCC1)NC(c1nc(C24CC5CC(CC(C5)C2)C4)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
CHEMBL3775851 145411 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 456 3 3 3 5.7 c1ccc2c3c([nH]c2c1)C(C1CCOCC1)NC(c1nc(C24CC5CC(CC(C5)C2)C4)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
49865343 22681 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST3 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST3 receptor expressed in human CCL39 cells by autoradiography
ChEMBL 1147 20 12 13 2.2 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cc3ccccc3[nH]2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(OC(=O)c3ccccc3)cc2)C(=O)N1 10.1021/jm1005868
CHEMBL1223228 22681 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST3 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST3 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
122179449 128224 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 397 3 2 2 6.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)O3)n2)cc1 10.1021/ml500514w
CHEMBL3582309 128224 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 397 3 2 2 6.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)O3)n2)cc1 10.1021/ml500514w
16737814 92282 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL227212 92282 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL504838 92282 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
16737814 92282 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST3 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST3 receptor
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
CHEMBL227212 92282 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST3 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST3 receptor
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
CHEMBL504838 92282 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST3 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST3 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
42637563 202289 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 989 12 9 12 2.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc3ccc(O)cc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL553656 202289 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 989 12 9 12 2.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc3ccc(O)cc3)NC2=O)cc1 10.1021/jm801314f
42637136 203283 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1074 15 10 13 1.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL563462 203283 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1074 15 10 13 1.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL387005 219182 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL None None None CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3I)C(=O)N[C@H]3CCCCNC(=O)CC[C@@H](NC(=O)[C@@H](Cc4ccccc4)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC3=O)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049519m
CHEMBL451932 220752 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
127033870 145311 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 430 3 2 4 5.1 Cn1c2c(c3ccccc31)C[C@H](c1nc(-c3ccc(F)cc3)c[nH]1)N[C@@H]2C1CCOCC1 10.1016/j.bmcl.2016.02.022
CHEMBL3775120 145311 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 430 3 2 4 5.1 Cn1c2c(c3ccccc31)C[C@H](c1nc(-c3ccc(F)cc3)c[nH]1)N[C@@H]2C1CCOCC1 10.1016/j.bmcl.2016.02.022
127030226 145399 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 466 3 3 3 5.9 FC(F)(F)c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775793 145399 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 466 3 3 3 5.9 FC(F)(F)c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
25189054 19476 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 685 11 4 6 3.0 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCN(S(=O)(=O)c3ccccc3)CC2)C1=O 10.1021/jm801205x
CHEMBL1187568 19476 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 685 11 4 6 3.0 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCN(S(=O)(=O)c3ccccc3)CC2)C1=O 10.1021/jm801205x
CHEMBL509513 19476 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 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
CHEMBL3350893 218294 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
CHEMBL3350886 218288 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
CHEMBL2079559 215974 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
44368398 17038 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1196 16 15 16 -0.2 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1161331 17038 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 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
CHEMBL265846 217446 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 3.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 3.
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+
CHEMBL502511 220934 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
127033872 145415 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 416 3 3 3 5.1 Fc1ccc(-c2cc([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)[nH]n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775922 145415 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 416 3 3 3 5.1 Fc1ccc(-c2cc([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)[nH]n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL412629 219791 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 3.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 3.
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+
127033874 145378 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 417 3 3 4 4.4 Fc1ccc(-c2n[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775625 145378 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 417 3 3 4 4.4 Fc1ccc(-c2n[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL428799 220250 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 3.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 3.
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm010037+
CHEMBL2079558 215973 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
122179457 128232 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 495 4 3 8 3.7 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml500514w
CHEMBL3582317 128232 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 495 4 3 8 3.7 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml500514w
122179478 128255 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 539 6 3 9 3.7 CCn1cc([C@@]2(c3nn(CC)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582339 128255 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 539 6 3 9 3.7 CCn1cc([C@@]2(c3nn(CC)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
13690207 122160 0 None - 5 Mouse 8.5 pIC50 = 8.5 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm960850i
CHEMBL3350037 122160 0 None - 5 Mouse 8.5 pIC50 = 8.5 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3
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
CHEMBL2371085 216790 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 3 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
16129706 215810 40 None -4 5 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm200307v
CHEMBL1823872 215810 40 None -4 5 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst3 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
CHEMBL1907758 215847 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=5)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 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
16129706 215810 40 None -4 5 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[LTT]-SS28 from human SST3 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST3 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysis
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.ejmech.2013.12.003
CHEMBL1823872 215810 40 None -4 5 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[LTT]-SS28 from human SST3 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST3 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
CHEMBL442494 220692 0 None -4 5 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
16129706 215810 40 None -4 5 Human 8.5 pIC50 = 8.5 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm049519m
CHEMBL1823872 215810 40 None -4 5 Human 8.5 pIC50 = 8.5 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3
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
118710528 120475 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cncc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
CHEMBL3323077 120475 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1cncc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
CHEMBL2371060 216786 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 3 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
CHEMBL408338 219485 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm049520l
CHEMBL409100 219525 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 3.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 3.
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+
CHEMBL1907758 215847 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
122179471 128247 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 524 6 4 9 3.9 CCn1cc([C@@]2(c3nnc(NC)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582331 128247 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 524 6 4 9 3.9 CCn1cc([C@@]2(c3nnc(NC)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
122179457 128232 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 495 4 3 8 3.7 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL3582317 128232 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 495 4 3 8 3.7 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL442494 220692 0 None -4 5 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst3 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm070886i
CHEMBL442494 220692 0 None -4 5 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST3 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST3 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
CHEMBL442494 220692 0 None -4 5 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3
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 220692 0 None -4 5 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
25189052 19444 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 676 10 5 6 3.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C1=O 10.1021/jm801205x
CHEMBL1187345 19444 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 676 10 5 6 3.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C1=O 10.1021/jm801205x
CHEMBL499681 19444 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 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
118710531 120478 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Displacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cccc(C(=O)O)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323080 120478 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Displacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from mouse SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cccc(C(=O)O)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL503036 220939 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
25188220 19263 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 11 4 4 4.2 C[C@H](NC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O)c1ccccc1 10.1021/jm801205x
CHEMBL1186489 19263 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 11 4 4 4.2 C[C@H](NC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O)c1ccccc1 10.1021/jm801205x
CHEMBL466609 19263 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 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
CHEMBL2011464 215891 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human sst3 by in vitro receptor autoradiography assayBinding affinity to human sst3 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
10577746 214031 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration required for somatostatin 3 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 3 receptor in radioligand binding assay ([125I]Tyr11-SRIF)
ChEMBL 514 8 3 4 4.6 NCCCC[C@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)SCCN(Cc2cccc3ccccc23)C1=O 10.1016/s0960-894x(00)00552-7
CHEMBL92914 214031 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration required for somatostatin 3 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 3 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
CHEMBL506892 220995 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
CHEMBL406197 219377 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL None None None CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(N)=O)CSSC[C@@H](N)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049520l
45267999 202468 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 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
CHEMBL556735 202468 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 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
CHEMBL2079559 215974 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
25187953 19461 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 725 10 4 6 3.8 CS(=O)(=O)N1CC2(CCN(C(=O)N[C@@H]3Cc4c([nH]c5ccccc45)CN([C@@H](CCCCN)C(=O)NCc4ccccc4)C3=O)CC2)c2ccccc21 10.1021/jm801205x
CHEMBL1187458 19461 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 725 10 4 6 3.8 CS(=O)(=O)N1CC2(CCN(C(=O)N[C@@H]3Cc4c([nH]c5ccccc45)CN([C@@H](CCCCN)C(=O)NCc4ccccc4)C3=O)CC2)c2ccccc21 10.1021/jm801205x
CHEMBL503379 19461 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 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
44368398 17038 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1196 16 15 16 -0.2 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1161331 17038 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 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
CHEMBL387458 219189 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 3 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
CHEMBL3350726 218270 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)c(I)c2)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL3350880 218282 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
CHEMBL524327 222381 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
70683416 80742 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1170 16 9 12 4.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL2021544 80742 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1170 16 9 12 4.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
127031456 145261 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 412 3 3 3 5.2 Cc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3774791 145261 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 412 3 3 3 5.2 Cc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3350897 218298 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
CHEMBL2372603 217053 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=2)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=2)
ChEMBL None None None C[C@H](O)[C@@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
CHEMBL511086 222371 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
127032661 145303 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 418 3 3 4 5.3 Cc1csc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
CHEMBL3775055 145303 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 418 3 3 4 5.3 Cc1csc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
127030227 145346 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 414 3 4 4 4.6 Oc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775398 145346 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 414 3 4 4 4.6 Oc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL510901 222369 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
45268875 202389 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1363 19 12 15 2.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3I)CSSC[C@@H](C(=O)N[C@@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL555977 202389 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1363 19 12 15 2.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3I)CSSC[C@@H](C(=O)N[C@@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL386023 219152 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL414571 219923 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 3.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 3.
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm010037+
CHEMBL447658 220731 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
CHEMBL3350884 218286 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
70688793 83633 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 454 3 4 3 4.5 CNC(=O)N1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL2069513 83633 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 454 3 4 3 4.5 CNC(=O)N1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL3350881 218283 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
90663867 113512 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)
ChEMBL 1322 20 18 20 -3.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)c(I)c2)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O)[C@@H]2O)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm040794i
CHEMBL3144279 113512 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 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
CHEMBL455760 220787 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst3 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst3 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
CHEMBL453936 220769 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
11563877 171499 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR3 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR3 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 668 9 3 5 5.7 Cc1cc(F)ccc1N1CCN(C(=O)N[C@@H](C(=O)Nc2cc(CN(C)C)ccc2OC(F)(F)F)[C@@H](C)c2c[nH]c3ccccc23)CC1=O 10.1016/j.bmc.2017.09.031
CHEMBL4217405 171499 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR3 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR3 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
127033555 145326 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 423 3 3 4 4.8 N#Cc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
CHEMBL3775241 145326 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 423 3 3 4 4.8 N#Cc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
CHEMBL3349676 218238 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
CHEMBL504087 220952 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
CHEMBL219375 216192 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst3Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst3
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
46902023 23810 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]iodotyrosyl from human SST3 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST3 receptor expressed in CHO cells
ChEMBL 544 11 3 7 3.7 COC[C@H]1O[C@@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCN)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254476 23810 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]iodotyrosyl from human SST3 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST3 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
CHEMBL3350883 218285 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
CHEMBL426698 220127 0 None - 0 Human 6.4 pIC50 = 6.4 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 3.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 3.
ChEMBL None None None CC(C)CNCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm010037+
118718854 122194 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350354 122194 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 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
CHEMBL526498 222466 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
CHEMBL386768 219168 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)
ChEMBL None None None None 10.1021/jm040794i
127030547 145391 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 417 3 3 4 4.4 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)nc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775734 145391 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 417 3 3 4 4.4 Fc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)nc1 10.1016/j.bmcl.2016.02.022
CHEMBL219375 216192 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst3 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst3 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 216192 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 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
CHEMBL216992 216127 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 3Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3
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
70697098 83623 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@H](C4CCOCC4)N3)n2)cc1 10.1021/ml200272z
CHEMBL2069503 83623 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@H](C4CCOCC4)N3)n2)cc1 10.1021/ml200272z
127029888 145350 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 474 4 3 3 6.6 c1ccc(-c2ccc(-c3c[nH]c([C@H]4Cc5c([nH]c6ccccc56)[C@@H](C5CCOCC5)N4)n3)cc2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775414 145350 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 474 4 3 3 6.6 c1ccc(-c2ccc(-c3c[nH]c([C@H]4Cc5c([nH]c6ccccc56)[C@@H](C5CCOCC5)N4)n3)cc2)cc1 10.1016/j.bmcl.2016.02.022
90663875 113518 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)
ChEMBL 1424 23 18 21 -2.3 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CCS[C@@H]2O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3144287 113518 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 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
25204216 83632 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 455 3 3 4 5.0 COC(=O)N1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL2069512 83632 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 455 3 3 4 5.0 COC(=O)N1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
71462984 90438 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 412 3 3 4 4.4 Cn1cc([C@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
CHEMBL2204942 90438 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 412 3 3 4 4.4 Cn1cc([C@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
CHEMBL442494 220692 0 None -4 5 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 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
122179474 128250 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 511 4 3 9 2.7 Cn1cc([C@@]2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582334 128250 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 511 4 3 9 2.7 Cn1cc([C@@]2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL2369533 216411 0 None - 0 Human 8.4 pIC50 = 8.4 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 3.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 3.
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+
118710531 120478 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cccc(C(=O)O)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323080 120478 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3cccc(C(=O)O)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL500326 220890 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
53311297 137336 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.
ChEMBL 499 4 3 7 4.4 Cc1nnc(C2(C3CCCO3)N[C@@H](c3nc(-c4ccc(F)c(C)n4)c[nH]3)Cc3c2[nH]c2ccccc32)o1 nan
CHEMBL3680936 137336 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.
ChEMBL 499 4 3 7 4.4 Cc1nnc(C2(C3CCCO3)N[C@@H](c3nc(-c4ccc(F)c(C)n4)c[nH]3)Cc3c2[nH]c2ccccc32)o1 nan
127030229 145296 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 428 4 3 4 4.9 COc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
CHEMBL3775031 145296 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 428 4 3 4 4.9 COc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
122179450 128225 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 422 3 3 2 5.8 CC1(c2ccccc2)N[C@@H](c2nc(-c3ccc(F)cc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/ml500514w
CHEMBL3582310 128225 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 422 3 3 2 5.8 CC1(c2ccccc2)N[C@@H](c2nc(-c3ccc(F)cc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/ml500514w
122179465 128241 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 509 5 3 8 4.0 CCc1nnc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)o1 10.1021/ml500514w
CHEMBL3582325 128241 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 509 5 3 8 4.0 CCc1nnc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)o1 10.1021/ml500514w
122179472 128248 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 538 6 3 9 3.9 CCn1cc([C@@]2(c3nnc(N(C)C)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582332 128248 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 538 6 3 9 3.9 CCn1cc([C@@]2(c3nnc(N(C)C)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
71457622 90428 0 None - 0 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 412 3 3 4 4.4 Cn1cc([C@@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
CHEMBL2204931 90428 0 None - 0 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 412 3 3 4 4.4 Cn1cc([C@@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
118710526 120473 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccnc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
CHEMBL3323075 120473 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 561 6 3 7 5.2 CCOC(=O)c1ccnc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)c1 10.1021/ml500028c
CHEMBL1907758 215847 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 3 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
122179464 128240 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 495 4 3 8 3.7 Cc1nnc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)o1 10.1021/ml500514w
CHEMBL3582324 128240 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 495 4 3 8 3.7 Cc1nnc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)o1 10.1021/ml500514w
122179482 128260 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 569 7 4 10 2.7 CCn1cc([C@@]2(c3nn(CC(=O)O)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582343 128260 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 569 7 4 10 2.7 CCn1cc([C@@]2(c3nn(CC(=O)O)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL2372713 217063 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity of human Somatostatin receptor type 3 (hsst3) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 3 (hsst3) 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
25188496 19307 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 476 9 3 5 2.5 COC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1186630 19307 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 476 9 3 5 2.5 COC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL473160 19307 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 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
118719275 122259 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3351044 122259 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL2371070 216787 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 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
25188218 19336 1 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 11 4 4 4.2 C[C@@H](NC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O)c1ccccc1 10.1021/jm801205x
CHEMBL1186753 19336 1 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 11 4 4 4.2 C[C@@H](NC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O)c1ccccc1 10.1021/jm801205x
CHEMBL476240 19336 1 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 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
CHEMBL3349675 218237 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
118710537 120485 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3ccc(C(=O)O)cn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323087 120485 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3ccc(C(=O)O)cn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
42637632 67049 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1334 20 11 14 5.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL174206 67049 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1334 20 11 14 5.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
127030531 145356 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 482 4 3 4 5.8 FC(F)(F)Oc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
CHEMBL3775456 145356 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 482 4 3 4 5.8 FC(F)(F)Oc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
68306176 137334 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.
ChEMBL 473 6 3 7 4.0 CCOC[C@]1(c2nnc(C)o2)N[C@@H](c2nc(-c3ccc(F)cn3)c[nH]2)Cc2c1[nH]c1ccccc21 nan
CHEMBL3680934 137334 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.Binding Scintillation Proximity Assay: The receptor-ligand binding Scintillation Proximity Assay (SPA) (N. D. Cook. Drug Discovery Today 1 (1996), pp. 287-294) for SSTR3 was performed with membranes isolated from Chinese hamster ovary (CHO)-K1 cells stably expressing the cloned human somatostatin receptors. Binding assays were performed in 384 well format using 125I-SS14 as the radioligand for SSTR3. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 mM MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL). CHO-K1 cell membranes were prebound to SPA beads and incubated with unlabelled test compounds and radiolabeled somatostatin in assay buffer. After 5 hours at room temperature, cpm/well was determined. Test compounds were examined in 10 point titrations over a range of concentrations from 0.00001 nM to 1200 nM. Percent inhibition was determined for each data point using binding in the presence of DMSO as the maximum achievable value.
ChEMBL 473 6 3 7 4.0 CCOC[C@]1(c2nnc(C)o2)N[C@@H](c2nc(-c3ccc(F)cn3)c[nH]2)Cc2c1[nH]c1ccccc21 nan
11678313 23787 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]iodotyrosyl from human SST3 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST3 receptor expressed in CHO cells
ChEMBL 542 12 3 7 3.6 COC[C@H]1O[C@@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254235 23787 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]iodotyrosyl from human SST3 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST3 receptor expressed in CHO cells
ChEMBL 542 12 3 7 3.6 COC[C@H]1O[C@@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL3349667 218230 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
70684550 83631 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 475 4 3 4 4.2 CS(=O)(=O)N1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL2069511 83631 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 475 4 3 4 4.2 CS(=O)(=O)N1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL438630 220563 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)O)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/jm049519m
CHEMBL412624 219790 0 None - 0 Human 6.4 pIC50 = 6.4 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 3.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 3.
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)O)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+
118718854 122194 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350354 122194 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350907 218305 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 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
CHEMBL505496 220972 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
70690870 83624 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 3 3 3 4.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCOC4)N3)n2)cc1 10.1021/ml200272z
CHEMBL2069504 83624 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 3 3 3 4.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCOC4)N3)n2)cc1 10.1021/ml200272z
44560863 195085 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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 195085 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
CHEMBL455435 220782 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst3 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst3 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
44368398 17038 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1196 16 15 16 -0.2 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1161331 17038 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 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
42637283 202293 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1334 20 11 14 5.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL553672 202293 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1334 20 11 14 5.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL3349671 218233 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
127033873 145299 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 398 3 3 3 4.9 c1ccc(-c2nc([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)c[nH]2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775037 145299 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 398 3 3 3 4.9 c1ccc(-c2nc([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)c[nH]2)cc1 10.1016/j.bmcl.2016.02.022
90663869 113514 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)
ChEMBL 1424 23 18 21 -2.3 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CCS[C@@H]2O[C@@H](CO)[C@H](O)[C@H](O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3144281 113514 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 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
122179467 128243 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 511 5 4 9 3.6 CCn1cc([C@@]2(c3nnc(O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582327 128243 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 511 5 4 9 3.6 CCn1cc([C@@]2(c3nnc(O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3349616 218221 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
122179470 128246 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 496 4 4 9 3.0 Cn1cc([C@@]2(c3nnc(N)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582330 128246 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 496 4 4 9 3.0 Cn1cc([C@@]2(c3nnc(N)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
25189325 19218 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 12 4 4 3.6 NCCCC[C@@H](C(=O)NCCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1186056 19218 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 12 4 4 3.6 NCCCC[C@@H](C(=O)NCCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL447455 19218 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 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
CHEMBL524870 222404 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
CHEMBL448431 220736 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
52948630 23777 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]iodotyrosyl from human SST3 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST3 receptor expressed in CHO cells
ChEMBL 542 12 3 7 3.6 COC[C@H]1O[C@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN)[C@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254140 23777 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]iodotyrosyl from human SST3 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST3 receptor expressed in CHO cells
ChEMBL 542 12 3 7 3.6 COC[C@H]1O[C@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN)[C@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL385811 219147 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(N)=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/jm049520l
CHEMBL414749 219932 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 3.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 3.
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm010037+
CHEMBL1909006 215854 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](N)Cc3ccccc3)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC2=O)cc1 10.1021/jm801314f
CHEMBL538948 215854 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](N)Cc3ccccc3)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC2=O)cc1 10.1021/jm801314f
25188780 19203 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 489 10 4 4 2.4 CC(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)NCCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1185941 19203 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 489 10 4 4 2.4 CC(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)NCCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL442605 19203 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 489 10 4 4 2.4 CC(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)NCCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL386784 219171 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3
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
CHEMBL3349612 218218 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
CHEMBL3350885 218287 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
CHEMBL525397 222424 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
122179455 128230 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 398 3 3 4 4.9 c1ccc2c3c([nH]c2c1)C(C1CCCCC1)N[C@@H](c1nc(-c2cnccn2)c[nH]1)C3 10.1021/ml500514w
CHEMBL3582315 128230 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 398 3 3 4 4.9 c1ccc2c3c([nH]c2c1)C(C1CCCCC1)N[C@@H](c1nc(-c2cnccn2)c[nH]1)C3 10.1021/ml500514w
44388123 175965 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL 1681 21 18 21 0.2 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3I)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL440618 175965 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL 1681 21 18 21 0.2 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3I)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL3349598 218206 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
25187681 19241 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 613 11 4 4 5.3 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccc(-c3ccccc3)cc2)C1=O 10.1021/jm801205x
CHEMBL1186190 19241 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 613 11 4 4 5.3 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccc(-c3ccccc3)cc2)C1=O 10.1021/jm801205x
CHEMBL453412 19241 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 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
CHEMBL509192 222113 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
CHEMBL376703 219033 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst3Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst3
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
CHEMBL3350895 218296 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
127033871 145409 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 412 3 3 3 5.2 Cc1[nH]c([C@H]2Cc3c([nH]c4ccccc34)[C@@H](C3CCOCC3)N2)nc1-c1ccccc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775846 145409 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 412 3 3 3 5.2 Cc1[nH]c([C@H]2Cc3c([nH]c4ccccc34)[C@@H](C3CCOCC3)N2)nc1-c1ccccc1 10.1016/j.bmcl.2016.02.022
11159133 122240 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1152 15 15 15 0.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
CHEMBL3350904 122240 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
CHEMBL261895 217299 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 3 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
CHEMBL505128 220967 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
CHEMBL501776 220923 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
CHEMBL2371051 216783 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0302445
CHEMBL1824056 215819 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst3 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
127034428 145304 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 495 4 3 8 3.7 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL3775061 145304 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 495 4 3 8 3.7 Cc1nc([C@@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
71462984 90438 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 412 3 3 4 4.4 Cn1cc([C@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
CHEMBL2204942 90438 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 412 3 3 4 4.4 Cn1cc([C@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
CHEMBL555737 222510 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm801314f
CHEMBL2111200 215994 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 3 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
127034125 145390 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 412 3 3 3 5.1 CC1(c2nc(-c3ccccc3)c[nH]2)Cc2c([nH]c3ccccc23)C(C2CCOCC2)N1 10.1016/j.bmcl.2016.02.022
CHEMBL3775729 145390 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 412 3 3 3 5.1 CC1(c2nc(-c3ccccc3)c[nH]2)Cc2c([nH]c3ccccc23)C(C2CCOCC2)N1 10.1016/j.bmcl.2016.02.022
162651887 187050 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR3 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR3 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 187050 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR3 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR3 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
CHEMBL414446 219910 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 3 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
CHEMBL446077 220722 0 None -9 3 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
91936728 168506 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=7)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=7)
ChEMBL None None None None 10.1021/jm040794i
CHEMBL413647 168506 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=7)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=7)
ChEMBL None None None None 10.1021/jm040794i
CHEMBL413419 219844 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3I)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL1909004 215853 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC(=O)[C@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm801314f
CHEMBL559022 215853 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC(=O)[C@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm801314f
CHEMBL263340 217347 0 None - 0 Human 6.2 pIC50 = 6.2 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 3.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 3.
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm010037+
CHEMBL3349674 218236 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
CHEMBL410144 219580 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)O)N(C)C(=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/jm049520l
11343811 122239 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1152 15 15 15 0.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
CHEMBL3350903 122239 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
CHEMBL3350909 218307 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
70690870 83624 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 3 3 3 4.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCOC4)N3)n2)cc1 10.1021/ml200272z
CHEMBL2069504 83624 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 3 3 3 4.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCOC4)N3)n2)cc1 10.1021/ml200272z
70697099 83629 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 397 3 4 3 4.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCNCC4)N3)n2)cc1 10.1021/ml200272z
CHEMBL2069509 83629 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 397 3 4 3 4.5 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCNCC4)N3)n2)cc1 10.1021/ml200272z
CHEMBL405784 219358 0 None - 0 Human 6.2 pIC50 = 6.2 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 3.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 3.
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)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+
11642413 23872 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]iodotyrosyl from human SST3 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST3 receptor expressed in CHO cells
ChEMBL 544 11 3 7 3.9 CS[C@@H]1O[C@H](COCc2ccc(Cl)cc2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCN 10.1021/jm1002777
CHEMBL1254967 23872 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]iodotyrosyl from human SST3 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST3 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
127030530 145338 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 482 4 3 4 5.8 FC(F)(F)Oc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3775316 145338 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 482 4 3 4 5.8 FC(F)(F)Oc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3349505 218189 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
CHEMBL3349672 218234 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
11457521 122237 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1136 15 14 14 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL3350892 122237 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
CHEMBL447177 220727 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
CHEMBL3350357 218254 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL2371108 216792 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 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
CHEMBL3349678 218240 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
42637069 202288 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1074 15 10 13 1.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL553655 202288 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL 1074 15 10 13 1.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL504248 220954 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
CHEMBL504462 220958 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
16738359 143961 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 641 13 4 4 5.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL374833 143961 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 641 13 4 4 5.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL453938 143961 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 641 13 4 4 5.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm801205x
16738359 143961 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST3 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST3 receptor
ChEMBL 641 13 4 4 5.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm070246f
CHEMBL374833 143961 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST3 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST3 receptor
ChEMBL 641 13 4 4 5.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm070246f
CHEMBL453938 143961 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST3 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST3 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
CHEMBL407649 219453 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 3 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
70682466 83628 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 497 3 3 4 6.1 CC(C)(C)OC(=O)N1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL2069508 83628 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from human SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 497 3 3 4 6.1 CC(C)(C)OC(=O)N1CCC(C2N[C@@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)CC1 10.1021/ml200272z
CHEMBL1907758 215847 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 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
CHEMBL504457 220956 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst3 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
71457622 90428 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 412 3 3 4 4.4 Cn1cc([C@@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
CHEMBL2204931 90428 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 412 3 3 4 4.4 Cn1cc([C@@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml300063m
122179468 128244 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 527 5 4 9 4.2 CCn1cc([C@@]2(c3nnc(S)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582328 128244 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 527 5 4 9 4.2 CCn1cc([C@@]2(c3nnc(S)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
118710536 120484 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3ccc(C(=O)O)cn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3323086 120484 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 533 5 4 6 4.7 Cn1cc([C@@]2(c3ccc(C(=O)O)cn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL1908982 215850 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC2=O)cc1 10.1021/jm801314f
CHEMBL552988 215850 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC2=O)cc1 10.1021/jm801314f
CHEMBL438776 220577 0 None - 0 Human 6.2 pIC50 = 6.2 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 3.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 3.
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)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+
CHEMBL554624 222505 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](N)Cc3ccccc3)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
118710533 120481 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3cc(C(=O)O)ccn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323083 120481 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3cc(C(=O)O)ccn3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
118718854 122194 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350354 122194 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350902 218302 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 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
CHEMBL3349614 218220 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
127030548 145280 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 433 3 3 4 5.0 Clc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)nc1 10.1016/j.bmcl.2016.02.022
CHEMBL3774909 145280 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 433 3 3 4 5.0 Clc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)nc1 10.1016/j.bmcl.2016.02.022
118710532 120479 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3cccc(C(=O)O)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL3323081 120479 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzerDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer
ChEMBL 533 5 4 6 4.7 Cn1cc([C@]2(c3cccc(C(=O)O)n3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500028c
CHEMBL1824058 215821 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst3 receptor in CCL39 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2cn(Cc3ccccc3)cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm200307v
CHEMBL3350888 218290 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030246p
CHEMBL3350888 218290 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
71460000 86434 0 None - 0 Human 6.1 pIC50 = 6.1 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 3.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 3.
ChEMBL 1644 25 18 20 1.9 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](CCCCN)NC(=O)[C@H](NC(=O)CCc3ccc(O)cc3)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+
CHEMBL2115143 86434 0 None - 0 Human 6.1 pIC50 = 6.1 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 3.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 3.
ChEMBL 1644 25 18 20 1.9 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](CCCCN)NC(=O)[C@H](NC(=O)CCc3ccc(O)cc3)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+
90663873 113516 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)
ChEMBL 1498 23 21 25 -5.1 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3144283 113516 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)
ChEMBL 1498 23 21 25 -5.1 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3144285 113516 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 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
59411406 128254 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 525 5 3 9 3.2 CCn1cc(C2(c3nn(C)c(=O)o3)NC(c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582338 128254 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 525 5 3 9 3.2 CCn1cc(C2(c3nn(C)c(=O)o3)NC(c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
156009460 185004 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL 1667 22 20 21 0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCCCCC[C@@H](NC(=O)[C@@H](Cc4ccccc4)NC(=O)[C@@H]([C@@H](C)O)NC2=O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)O)CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc2ccccc2)C(=O)N3)cc1 10.1021/jm049519m
CHEMBL4649897 185004 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL 1667 22 20 21 0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCCCCC[C@@H](NC(=O)[C@@H](Cc4ccccc4)NC(=O)[C@@H]([C@@H](C)O)NC2=O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)O)CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc2ccccc2)C(=O)N3)cc1 10.1021/jm049519m
11389178 122238 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1136 15 14 14 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL3350900 122238 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
127031771 145292 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 400 3 3 5 3.7 c1ccc2c3c([nH]c2c1)[C@@H](C1CCOCC1)N[C@@H](c1nc(-c2cnccn2)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
CHEMBL3775018 145292 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 400 3 3 5 3.7 c1ccc2c3c([nH]c2c1)[C@@H](C1CCOCC1)N[C@@H](c1nc(-c2cnccn2)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
127031773 145288 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 405 3 3 5 4.4 c1ccc2c3c([nH]c2c1)[C@@H](C1CCOCC1)N[C@@H](c1nc(-c2cscn2)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
CHEMBL3774986 145288 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 405 3 3 5 4.4 c1ccc2c3c([nH]c2c1)[C@@H](C1CCOCC1)N[C@@H](c1nc(-c2cscn2)c[nH]1)C3 10.1016/j.bmcl.2016.02.022
CHEMBL559150 222523 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst3 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm801314f
CHEMBL265836 217445 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049519m
127031432 145344 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 429 4 3 5 4.3 COc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)n1 10.1016/j.bmcl.2016.02.022
CHEMBL3775387 145344 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 429 4 3 5 4.3 COc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)n1 10.1016/j.bmcl.2016.02.022
CHEMBL262379 217317 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3
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
127031454 145273 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 432 3 3 3 5.6 Clc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
CHEMBL3774866 145273 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 432 3 3 3 5.6 Clc1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1016/j.bmcl.2016.02.022
71452297 90430 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 414 3 3 5 4.4 Cc1nc([C@@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204933 90430 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 414 3 3 5 4.4 Cc1nc([C@@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
127031154 145266 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 416 3 3 3 5.1 Fc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
CHEMBL3774817 145266 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 416 3 3 3 5.1 Fc1cccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)c1 10.1016/j.bmcl.2016.02.022
CHEMBL3350911 218308 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
44560905 195605 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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 195605 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
57384077 83622 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]SS-14 from mouse SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from mouse SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml200272z
CHEMBL2069502 83622 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]SS-14 from mouse SST3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]SS-14 from mouse SST3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml200272z
57384077 83622 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml300063m
CHEMBL2069502 83622 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 398 3 3 3 4.9 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)[C@@H](C4CCOCC4)N3)n2)cc1 10.1021/ml300063m
CHEMBL437451 220499 0 None - 0 Human 7.1 pIC50 = 7.1 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 3.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 3.
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+
CHEMBL2011461 215888 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human sst3 by in vitro receptor autoradiography assayBinding affinity to human sst3 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
CHEMBL3349610 218216 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
90663874 113517 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)
ChEMBL 1660 26 24 30 -7.3 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O[C@@H]4O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]4O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3144286 113517 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)
ChEMBL 1660 26 24 30 -7.3 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O[C@@H]4O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]4O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3144291 113517 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 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
CHEMBL2111200 215994 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 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
44560866 195656 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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 195656 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
52941607 23797 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]iodotyrosyl from human SST3 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST3 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 23797 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]iodotyrosyl from human SST3 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST3 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
162646037 186293 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR3 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR3 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1387 27 17 19 -2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4741230 186293 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR3 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR3 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
44560873 195926 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiography
ChEMBL 1809 40 18 25 -1.0 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCOCCOCCOCCNC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL510793 195926 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
158782 164613 20 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=4)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=4)
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 164613 20 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=4)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 3 expressed in CCL39 cells; (n=4)
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
137062183 128238 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 497 4 4 9 3.1 Cn1cc([C@@]2(c3noc(O)n3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582322 128238 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 497 4 4 9 3.1 Cn1cc([C@@]2(c3noc(O)n3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3349508 218192 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
49865342 22680 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST3 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST3 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
CHEMBL1223227 22680 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST3 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST3 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
CHEMBL3350896 218297 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 3 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030246p
CHEMBL3350896 218297 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
25187955 19208 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 646 9 4 4 4.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCC3(CCc4ccccc43)CC2)C1=O 10.1021/jm801205x
CHEMBL1185951 19208 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 646 9 4 4 4.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCC3(CCc4ccccc43)CC2)C1=O 10.1021/jm801205x
CHEMBL443084 19208 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 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
71452297 90430 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 414 3 3 5 4.4 Cc1nc([C@@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
CHEMBL2204933 90430 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins
ChEMBL 414 3 3 5 4.4 Cc1nc([C@@H]2N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1021/ml300063m
127034426 145394 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 477 4 3 8 3.6 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccccn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL3775760 145394 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 477 4 3 8 3.6 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccccn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL406373 219385 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 3 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
CHEMBL501282 220915 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
44388122 88918 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL 1555 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL216789 88918 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL 1555 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL3349665 218228 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
CHEMBL438285 220543 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049519m
25188776 19254 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 551 11 4 4 3.6 NCCCC[C@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1186427 19254 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cells
ChEMBL 551 11 4 4 3.6 NCCCC[C@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL462020 19254 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 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
49865347 22685 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST3 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST3 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 22685 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST3 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST3 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
13690207 122160 0 None -30 5 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against human somatostatin receptor type 3 in CHO-K1 cellsInhibitory concentration against human somatostatin receptor type 3 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 10.1021/jm050376t
CHEMBL3350037 122160 0 None -30 5 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against human somatostatin receptor type 3 in CHO-K1 cellsInhibitory concentration against human somatostatin receptor type 3 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 10.1021/jm050376t
CHEMBL3349608 218215 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards cloned human somatostatin 3 (hsst) receptorBinding affinity towards cloned human somatostatin 3 (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
CHEMBL412029 219751 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst3Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst3
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
44388124 166149 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL 1680 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3I)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL410048 166149 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 3
ChEMBL 1680 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3I)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL436892 220471 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst3Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst3
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
CHEMBL498985 220868 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst3 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst3 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
CHEMBL413378 219842 0 None - 0 Human 6.0 pIC50 = 6.0 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 3.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 3.
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccc([N+](=O)[O-])cc3)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+
CHEMBL2011463 215890 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human sst3 by in vitro receptor autoradiography assayBinding affinity to human sst3 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
CHEMBL3122124 217882 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[LTT]-SS28 from human SST3 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST3 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
CHEMBL3350882 218284 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 3 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
2019 10447 0 None 1 10 Human 10.5 pKd = 10.5 Binding
Displacement of [125I]somatostatin from human SSTR3 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR3 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
44386062 10447 0 None 1 10 Human 10.5 pKd = 10.5 Binding
Displacement of [125I]somatostatin from human SSTR3 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR3 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
CHEMBL440072 10447 0 None 1 10 Human 10.5 pKd = 10.5 Binding
Displacement of [125I]somatostatin from human SSTR3 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR3 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
46880584 12310 0 None 758 2 Human 8.9 pKd = 8.9 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 620 9 0 9 4.4 COC(=O)c1cc(C[C@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)[C@H]3CCCC[C@H]3C2)cc(C(=O)OC)c1 10.1016/j.bmcl.2010.01.063
CHEMBL1076621 12310 0 None 758 2 Human 8.9 pKd = 8.9 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 620 9 0 9 4.4 COC(=O)c1cc(C[C@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)[C@H]3CCCC[C@H]3C2)cc(C(=O)OC)c1 10.1016/j.bmcl.2010.01.063
46880582 12321 0 None 295 2 Human 8.9 pKd = 8.9 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 620 9 0 9 4.4 COC(=O)c1cc(CC(C)CN2C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)[C@H]3CCCC[C@H]3C2)cc(C(=O)OC)c1 10.1016/j.bmcl.2010.01.063
CHEMBL1076659 12321 0 None 295 2 Human 8.9 pKd = 8.9 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 620 9 0 9 4.4 COC(=O)c1cc(CC(C)CN2C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)[C@H]3CCCC[C@H]3C2)cc(C(=O)OC)c1 10.1016/j.bmcl.2010.01.063
20597810 12331 0 None 245 2 Human 8.0 pKd = 8.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 547 6 0 5 5.2 C[C@@H](Cc1ccc2nccnc2c1)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
CHEMBL1076709 12331 0 None 245 2 Human 8.0 pKd = 8.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 547 6 0 5 5.2 C[C@@H](Cc1ccc2nccnc2c1)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
46880578 12317 0 None 83 2 Human 8.0 pKd = 8.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 548 7 0 7 4.6 CC(Cc1ccc2c(c1)OCO2)CN1C[C@H]2CCCC[C@H]2[C@@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1076655 12317 0 None 83 2 Human 8.0 pKd = 8.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 548 7 0 7 4.6 CC(Cc1ccc2c(c1)OCO2)CN1C[C@H]2CCCC[C@H]2[C@@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C1 10.1016/j.bmcl.2010.01.063
46880853 12337 0 None 147 2 Human 8.0 pKd = 8.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 536 6 0 5 5.4 C[C@@H](Cc1ccc2ocnc2c1)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
CHEMBL1076718 12337 0 None 147 2 Human 8.0 pKd = 8.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 536 6 0 5 5.4 C[C@@H](Cc1ccc2ocnc2c1)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
44564783 183704 0 None -1479 4 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 484 8 0 5 4.8 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2010.01.063
CHEMBL461988 183704 0 None -1479 4 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 484 8 0 5 4.8 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2010.01.063
46880590 12312 0 None -2 2 Human 7.0 pKd = 7.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 549 6 0 5 5.2 Cc1cn2cc(C[C@H](C)CN3C[C@@H](C(=O)N4CCN(c5ccc(F)c(F)c5)CC4)[C@H]4CCCC[C@H]4C3)ccc2n1 10.1016/j.bmcl.2010.01.063
CHEMBL1076627 12312 0 None -2 2 Human 7.0 pKd = 7.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 549 6 0 5 5.2 Cc1cn2cc(C[C@H](C)CN3C[C@@H](C(=O)N4CCN(c5ccc(F)c(F)c5)CC4)[C@H]4CCCC[C@H]4C3)ccc2n1 10.1016/j.bmcl.2010.01.063
46880581 12320 0 None 21 2 Human 7.0 pKd = 7.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 620 9 0 9 4.4 COC(=O)c1cc(CC(C)CN2C[C@H]3CCCC[C@H]3[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)C2)cc(C(=O)OC)c1 10.1016/j.bmcl.2010.01.063
CHEMBL1076658 12320 0 None 21 2 Human 7.0 pKd = 7.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 620 9 0 9 4.4 COC(=O)c1cc(CC(C)CN2C[C@H]3CCCC[C@H]3[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)C2)cc(C(=O)OC)c1 10.1016/j.bmcl.2010.01.063
46880819 12334 0 None - 1 Human 7.0 pKd = 7.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 556 6 0 8 4.0 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccc4nccnc4n3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1076715 12334 0 None - 1 Human 7.0 pKd = 7.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 556 6 0 8 4.0 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccc4nccnc4n3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL407209 219426 1 None -17 4 Human 8.0 pKd = 8.0 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)
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
CHEMBL408752 219509 0 None -77 4 Human 7.9 pKd = 7.9 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)
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
46880579 12318 0 None 5 2 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 548 7 0 7 4.6 CC(Cc1ccc2c(c1)OCO2)CN1C[C@H]2CCCC[C@H]2[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1076656 12318 0 None 5 2 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 548 7 0 7 4.6 CC(Cc1ccc2c(c1)OCO2)CN1C[C@H]2CCCC[C@H]2[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C1 10.1016/j.bmcl.2010.01.063
46880573 12868 0 None 1 2 Human 6.9 pKd = 6.9 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 510 6 0 5 5.2 O=C(C1CCCN(CCC2c3ccccc3-c3ccccc32)C1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.bmcl.2010.01.063
CHEMBL1080733 12868 0 None 1 2 Human 6.9 pKd = 6.9 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 510 6 0 5 5.2 O=C(C1CCCN(CCC2c3ccccc3-c3ccccc32)C1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.bmcl.2010.01.063
44565112 19531 0 None -1621 6 Human 5.9 pKd = 5.9 Binding
Binding affinity to human sst3 receptorBinding affinity to human sst3 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1187847 19531 0 None -1621 6 Human 5.9 pKd = 5.9 Binding
Binding affinity to human sst3 receptorBinding affinity to human sst3 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL523814 19531 0 None -1621 6 Human 5.9 pKd = 5.9 Binding
Binding affinity to human sst3 receptorBinding affinity to human sst3 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
46880576 12315 0 None 1 2 Human 5.9 pKd = 5.9 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 548 7 0 7 4.7 CC(Cc1ccc2c(c1)OCO2)CN1C[C@@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2CCCC[C@@H]21 10.1016/j.bmcl.2010.01.063
CHEMBL1076653 12315 0 None 1 2 Human 5.9 pKd = 5.9 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 548 7 0 7 4.7 CC(Cc1ccc2c(c1)OCO2)CN1C[C@@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2CCCC[C@@H]21 10.1016/j.bmcl.2010.01.063
CHEMBL265636 217437 0 None -8 4 Human 6.9 pKd = 6.9 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)
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
46880822 14264 0 None - 1 Human 5.9 pKd = 5.9 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 543 6 0 7 4.3 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cccc4nccn34)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1087113 14264 0 None - 1 Human 5.9 pKd = 5.9 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 543 6 0 7 4.3 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cccc4nccn34)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL405421 219339 0 None -12 4 Human 7.9 pKd = 7.9 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)
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
46880781 12328 0 None - 1 Human 5.9 pKd = 5.9 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 555 6 0 7 4.6 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cccc4nccnc34)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1076692 12328 0 None - 1 Human 5.9 pKd = 5.9 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 555 6 0 7 4.6 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cccc4nccnc34)CC2)C1 10.1016/j.bmcl.2010.01.063
46880855 12332 0 None 165 2 Human 7.9 pKd = 7.9 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 540 8 0 5 5.0 CCOc1ccc(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
CHEMBL1076710 12332 0 None 165 2 Human 7.9 pKd = 7.9 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 540 8 0 5 5.0 CCOc1ccc(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
46880577 12316 0 None 3 2 Human 6.8 pKd = 6.8 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 548 7 0 7 4.7 CC(Cc1ccc2c(c1)OCO2)CN1C[C@@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2010.01.063
CHEMBL1076654 12316 0 None 3 2 Human 6.8 pKd = 6.8 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 548 7 0 7 4.7 CC(Cc1ccc2c(c1)OCO2)CN1C[C@@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2010.01.063
46880820 12339 0 None - 1 Human 5.8 pKd = 5.8 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 556 6 0 8 4.0 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cc4nccnc4cn3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1076720 12339 0 None - 1 Human 5.8 pKd = 5.8 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 556 6 0 8 4.0 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cc4nccnc4cn3)CC2)C1 10.1016/j.bmcl.2010.01.063
46880575 12314 0 None 3 2 Human 6.8 pKd = 6.8 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 548 7 0 7 4.7 CC(Cc1ccc2c(c1)OCO2)CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2CCCC[C@@H]21 10.1016/j.bmcl.2010.01.063
CHEMBL1076652 12314 0 None 3 2 Human 6.8 pKd = 6.8 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 548 7 0 7 4.7 CC(Cc1ccc2c(c1)OCO2)CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2CCCC[C@@H]21 10.1016/j.bmcl.2010.01.063
44565159 201670 0 None -5011 5 Human 5.8 pKd = 5.8 Binding
Binding affinity to human sst3 receptorBinding affinity to human sst3 receptor
ChEMBL 497 7 0 7 4.5 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL540705 201670 0 None -5011 5 Human 5.8 pKd = 5.8 Binding
Binding affinity to human sst3 receptorBinding affinity to human sst3 receptor
ChEMBL 497 7 0 7 4.5 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL384836 219116 0 None 1 5 Human 7.8 pKd = 7.8 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)
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
CHEMBL407571 219448 0 None -17 4 Human 7.8 pKd = 7.8 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)
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
CHEMBL385409 219128 0 None -1 4 Human 7.7 pKd = 7.7 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)
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
46880783 13147 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 546 6 0 9 3.6 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccc4nonc4n3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1082179 13147 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 546 6 0 9 3.6 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccc4nonc4n3)CC2)C1 10.1016/j.bmcl.2010.01.063
155544425 180161 0 None -912 5 Human 7.7 pKd = 7.7 Binding
Displacement of [125I]somatostatin from human SSTR3 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR3 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL 1785 27 15 26 3.3 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSC[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc3ccccc3)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O)[C@@]1(C)O[C@H]1[C@H](C)[C@@H]1C[C@@](O)(NC(=O)O1)[C@H](OC)/C=C/C=C(\C)C2 10.1021/acs.jmedchem.8b02036
CHEMBL4527856 180161 0 None -912 5 Human 7.7 pKd = 7.7 Binding
Displacement of [125I]somatostatin from human SSTR3 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR3 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL 1785 27 15 26 3.3 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSC[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc3ccccc3)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O)[C@@]1(C)O[C@H]1[C@H](C)[C@@H]1C[C@@](O)(NC(=O)O1)[C@H](OC)/C=C/C=C(\C)C2 10.1021/acs.jmedchem.8b02036
46880782 13146 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 545 6 0 8 4.2 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccc4nonc4c3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1082178 13146 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 545 6 0 8 4.2 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccc4nonc4c3)CC2)C1 10.1016/j.bmcl.2010.01.063
46880780 13080 0 None - 1 Human 6.7 pKd = 6.7 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 561 6 0 8 4.7 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cccc4nsnc34)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1081836 13080 0 None - 1 Human 6.7 pKd = 6.7 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 561 6 0 8 4.7 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cccc4nsnc34)CC2)C1 10.1016/j.bmcl.2010.01.063
46880637 12876 0 None - 1 Human 6.7 pKd = 6.7 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 521 6 0 5 4.8 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1080754 12876 0 None - 1 Human 6.7 pKd = 6.7 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 521 6 0 5 4.8 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2010.01.063
46880583 12309 0 None 194 2 Human 8.7 pKd = 8.7 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 620 9 0 9 4.4 COC(=O)c1cc(C[C@@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)[C@H]3CCCC[C@H]3C2)cc(C(=O)OC)c1 10.1016/j.bmcl.2010.01.063
CHEMBL1076620 12309 0 None 194 2 Human 8.7 pKd = 8.7 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 620 9 0 9 4.4 COC(=O)c1cc(C[C@@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)[C@H]3CCCC[C@H]3C2)cc(C(=O)OC)c1 10.1016/j.bmcl.2010.01.063
CHEMBL405561 219345 0 None 3 4 Human 8.6 pKd = 8.6 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)
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
46880580 12319 0 None 346 2 Human 8.5 pKd = 8.5 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 620 9 0 9 4.4 COC(=O)c1cc(CC(C)CN2CC3CCCCC3C(C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)C2)cc(C(=O)OC)c1 10.1016/j.bmcl.2010.01.063
CHEMBL1076657 12319 0 None 346 2 Human 8.5 pKd = 8.5 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 620 9 0 9 4.4 COC(=O)c1cc(CC(C)CN2CC3CCCCC3C(C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)C2)cc(C(=O)OC)c1 10.1016/j.bmcl.2010.01.063
46880639 12999 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 539 6 0 5 5.0 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1081442 12999 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 539 6 0 5 5.0 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)C1 10.1016/j.bmcl.2010.01.063
44447073 101325 0 None -6309 10 Human 5.6 pKd = 5.6 Binding
Binding affinity to human recombinant sst3 receptorBinding affinity to human recombinant sst3 receptor
ChEMBL 534 2 1 6 3.8 CN1C[C@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL251835 101325 0 None -6309 10 Human 5.6 pKd = 5.6 Binding
Binding affinity to human recombinant sst3 receptorBinding affinity to human recombinant sst3 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
46880821 14249 0 None - 1 Human 6.6 pKd = 6.6 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 544 6 0 8 3.7 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccc4nccn4n3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1086988 14249 0 None - 1 Human 6.6 pKd = 6.6 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 544 6 0 8 3.7 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccc4nccn4n3)CC2)C1 10.1016/j.bmcl.2010.01.063
46880735 12708 0 None - 1 Human 5.6 pKd = 5.6 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 534 6 0 7 3.4 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cccc(=O)n3C)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1079799 12708 0 None - 1 Human 5.6 pKd = 5.6 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 534 6 0 7 3.4 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cccc(=O)n3C)CC2)C1 10.1016/j.bmcl.2010.01.063
46880851 14447 0 None - 1 Human 5.6 pKd = 5.6 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 544 6 0 8 3.7 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cccc4nncn34)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1088611 14447 0 None - 1 Human 5.6 pKd = 5.6 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 544 6 0 8 3.7 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cccc4nncn34)CC2)C1 10.1016/j.bmcl.2010.01.063
10162564 19312 0 None -4677 8 Human 5.6 pKd = 5.6 Binding
Binding affinity to human sst3 receptorBinding affinity to human sst3 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1186652 19312 0 None -4677 8 Human 5.6 pKd = 5.6 Binding
Binding affinity to human sst3 receptorBinding affinity to human sst3 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL473763 19312 0 None -4677 8 Human 5.6 pKd = 5.6 Binding
Binding affinity to human sst3 receptorBinding affinity to human sst3 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
46880856 12333 0 None 66 2 Human 7.5 pKd = 7.5 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 539 8 1 5 5.1 CCNc1ccc(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
CHEMBL1076711 12333 0 None 66 2 Human 7.5 pKd = 7.5 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 539 8 1 5 5.1 CCNc1ccc(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
17955460 183554 0 None -3630 9 Human 5.6 pKd = 5.6 Binding
Binding affinity to human sst3 receptorBinding affinity to human sst3 receptor
ChEMBL 491 7 0 4 5.3 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL460542 183554 0 None -3630 9 Human 5.6 pKd = 5.6 Binding
Binding affinity to human sst3 receptorBinding affinity to human sst3 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
CHEMBL2370168 216586 0 None -58 5 Human 6.6 pKd = 6.6 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst3) expressed in CHO cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst3) expressed in CHO cells.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCNC(=O)[C@@H](N)Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm970393l
9849682 101727 0 None -14454 10 Human 5.5 pKd = 5.5 Binding
Binding affinity to human recombinant sst3 receptorBinding affinity to human recombinant sst3 receptor
ChEMBL 523 2 1 5 2.9 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL254500 101727 0 None -14454 10 Human 5.5 pKd = 5.5 Binding
Binding affinity to human recombinant sst3 receptorBinding affinity to human recombinant sst3 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
CHEMBL413373 219841 0 None 3 4 Human 8.5 pKd = 8.5 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)
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
46865535 12311 0 None 67 7 Human 8.5 pKd = 8.5 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 550 6 0 5 5.7 Cc1nc2cc(C[C@H](C)CN3C[C@@H](C(=O)N4CCN(c5ccc(F)c(F)c5)CC4)[C@H]4CCCC[C@H]4C3)ccc2o1 10.1016/j.bmcl.2010.01.063
CHEMBL1076622 12311 0 None 67 7 Human 8.5 pKd = 8.5 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 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
44564857 185717 0 None -6 4 Human 6.5 pKd = 6.5 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 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.2010.01.063
CHEMBL470331 185717 0 None -6 4 Human 6.5 pKd = 6.5 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 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.2010.01.063
46880682 13074 0 None - 1 Human 6.5 pKd = 6.5 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 504 6 0 6 4.1 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1081804 13074 0 None - 1 Human 6.5 pKd = 6.5 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 504 6 0 6 4.1 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL2370166 216584 0 None -38 5 Human 6.5 pKd = 6.5 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst3) expressed in CHO cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst3) 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
46880854 12338 0 None 263 2 Human 7.5 pKd = 7.5 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 536 6 0 6 4.3 C[C@@H](Cc1ccc2ncnn2c1)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
CHEMBL1076719 12338 0 None 263 2 Human 7.5 pKd = 7.5 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 536 6 0 6 4.3 C[C@@H](Cc1ccc2ncnn2c1)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
46880588 20989 0 None -5 7 Human 5.4 pKd = 5.4 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@@H](C)CN2C[C@H]3CCCC[C@H]3[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)C2)cn1 10.1016/j.bmcl.2010.01.063
CHEMBL1076625 20989 0 None -5 7 Human 5.4 pKd = 5.4 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@@H](C)CN2C[C@H]3CCCC[C@H]3[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)C2)cn1 10.1016/j.bmcl.2010.01.063
CHEMBL1198974 20989 0 None -5 7 Human 5.4 pKd = 5.4 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 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
9871544 20988 3 None 1 11 Mouse 8.3 pKd = 8.3 Binding
Displacement of [125I]SRIF-28 from mouse recombinant SST3 receptorDisplacement of [125I]SRIF-28 from mouse recombinant SST3 receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)[C@H]3CCCC[C@H]3C2)cn1 10.1016/j.bmcl.2010.01.063
CHEMBL1076624 20988 3 None 1 11 Mouse 8.3 pKd = 8.3 Binding
Displacement of [125I]SRIF-28 from mouse recombinant SST3 receptorDisplacement of [125I]SRIF-28 from mouse recombinant SST3 receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)[C@H]3CCCC[C@H]3C2)cn1 10.1016/j.bmcl.2010.01.063
CHEMBL1198948 20988 3 None 1 11 Mouse 8.3 pKd = 8.3 Binding
Displacement of [125I]SRIF-28 from mouse recombinant SST3 receptorDisplacement of [125I]SRIF-28 from mouse recombinant SST3 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
CHEMBL2370167 216585 0 None -190 5 Human 6.4 pKd = 6.4 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst3) expressed in CHO cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst3) 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
46880683 13075 0 None - 1 Human 6.4 pKd = 6.4 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 538 6 0 6 4.7 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cccc(Cl)n3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1081805 13075 0 None - 1 Human 6.4 pKd = 6.4 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 538 6 0 6 4.7 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cccc(Cl)n3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL409019 219521 0 None -1 5 Human 7.4 pKd = 7.4 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)
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
CHEMBL437093 220484 0 None -7 5 Human 6.4 pKd = 6.4 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)
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
CHEMBL411017 219637 0 None -3 4 Human 7.3 pKd = 7.3 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)
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
CHEMBL421362 220053 0 None -151 5 Human 6.3 pKd = 6.3 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst3) expressed in CHO cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst3) 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
CHEMBL413830 219868 0 None -20 5 Human 6.3 pKd = 6.3 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)
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
44447077 101391 0 None -12 7 Human 5.3 pKd = 5.3 Binding
Binding affinity to human recombinant sst3 receptorBinding affinity to human recombinant sst3 receptor
ChEMBL 523 2 1 5 2.9 CN1C[C@@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@H]2c3cccc4[nH]c(Br)c(c34)C[C@@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252231 101391 0 None -12 7 Human 5.3 pKd = 5.3 Binding
Binding affinity to human recombinant sst3 receptorBinding affinity to human recombinant sst3 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
46880638 12998 0 None - 1 Human 7.2 pKd = 7.2 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 521 6 0 5 4.8 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1081441 12998 0 None - 1 Human 7.2 pKd = 7.2 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 521 6 0 5 4.8 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL412466 219771 0 None -36 4 Human 7.2 pKd = 7.2 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)
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
9871544 20988 3 None -1 11 Human 8.2 pKd = 8.2 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)[C@H]3CCCC[C@H]3C2)cn1 10.1016/j.bmcl.2010.01.063
CHEMBL1076624 20988 3 None -1 11 Human 8.2 pKd = 8.2 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)[C@H]3CCCC[C@H]3C2)cn1 10.1016/j.bmcl.2010.01.063
CHEMBL1198948 20988 3 None -1 11 Human 8.2 pKd = 8.2 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 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
46865536 18691 0 None 19 7 Human 8.1 pKd = 8.1 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 553 6 0 6 5.2 C[C@@H](Cc1ccc2nsnc2c1)CN1C[C@@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)[C@H]2CCCC[C@H]2C1 10.1016/j.bmcl.2010.01.063
CHEMBL1076623 18691 0 None 19 7 Human 8.1 pKd = 8.1 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 553 6 0 6 5.2 C[C@@H](Cc1ccc2nsnc2c1)CN1C[C@@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)[C@H]2CCCC[C@H]2C1 10.1016/j.bmcl.2010.01.063
CHEMBL1182658 18691 0 None 19 7 Human 8.1 pKd = 8.1 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 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
44447078 101392 0 None -39 7 Human 5.1 pKd = 5.1 Binding
Binding affinity to human recombinant sst3 receptorBinding affinity to human recombinant sst3 receptor
ChEMBL 534 2 1 6 3.8 CN1C[C@@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@H]2c3cccc4[nH]c(Br)c(c34)C[C@@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252232 101392 0 None -39 7 Human 5.1 pKd = 5.1 Binding
Binding affinity to human recombinant sst3 receptorBinding affinity to human recombinant sst3 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
46880685 12326 0 None - 1 Human 6.1 pKd = 6.1 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 572 6 0 6 5.1 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1076686 12326 0 None - 1 Human 6.1 pKd = 6.1 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 572 6 0 6 5.1 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)C1 10.1016/j.bmcl.2010.01.063
46880734 12707 0 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 529 6 0 7 3.9 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccc(C#N)cn3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1079798 12707 0 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 529 6 0 7 3.9 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccc(C#N)cn3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL438471 220552 0 None 6 4 Human 8.1 pKd = 8.1 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)
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
46880852 12336 0 None 107 2 Human 8.1 pKd = 8.1 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 539 6 0 5 5.0 C[C@@H](Cc1ccc2c(c1)OCO2)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
CHEMBL1076717 12336 0 None 107 2 Human 8.1 pKd = 8.1 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 539 6 0 5 5.0 C[C@@H](Cc1ccc2c(c1)OCO2)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
CHEMBL384164 219097 0 None -63 3 Human 6.1 pKd = 6.1 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)
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
46880574 12869 0 None 1 2 Human 7.1 pKd = 7.1 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 494 7 0 7 3.6 CC(Cc1ccc2c(c1)OCO2)CN1CCCC(C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1080734 12869 0 None 1 2 Human 7.1 pKd = 7.1 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 494 7 0 7 3.6 CC(Cc1ccc2c(c1)OCO2)CN1CCCC(C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C1 10.1016/j.bmcl.2010.01.063
2030 10444 10 None -12302 10 Human 5.1 pKd = 5.1 Binding
Binding affinity to human recombinant sst3 receptorBinding affinity to human recombinant sst3 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
5311377 10444 10 None -12302 10 Human 5.1 pKd = 5.1 Binding
Binding affinity to human recombinant sst3 receptorBinding affinity to human recombinant sst3 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
CHEMBL251541 10444 10 None -12302 10 Human 5.1 pKd = 5.1 Binding
Binding affinity to human recombinant sst3 receptorBinding affinity to human recombinant sst3 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
46880736 12743 0 None - 1 Human 7.0 pKd = 7.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 545 6 0 8 4.2 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cccc4nonc34)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1079969 12743 0 None - 1 Human 7.0 pKd = 7.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 545 6 0 8 4.2 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3cccc4nonc34)CC2)C1 10.1016/j.bmcl.2010.01.063
46880684 13076 0 None - 1 Human 7.0 pKd = 7.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 538 6 0 6 4.7 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccc(Cl)cn3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1081806 13076 0 None - 1 Human 7.0 pKd = 7.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 538 6 0 6 4.7 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccc(Cl)cn3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL386676 219165 0 None -2 4 Human 7.0 pKd = 7.0 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst3)
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
46880818 14248 0 None - 1 Human 7.0 pKd = 7.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 562 6 0 9 4.1 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C1 10.1016/j.bmcl.2010.01.063
CHEMBL1086987 14248 0 None - 1 Human 7.0 pKd = 7.0 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 562 6 0 9 4.1 CC(Cc1ccc2c(c1)OCO2)CN1CC2CCCCC2C(C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C1 10.1016/j.bmcl.2010.01.063
16129706 215810 40 None -4 5 Human 10.0 pKi = 10 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0108449
CHEMBL1823872 215810 40 None -4 5 Human 10.0 pKi = 10 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) 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
16129706 215810 40 None -4 5 Human 9.9 pKi = 9.9 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 receptor expressed in CHO cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/s0960-894x(01)00107-x
CHEMBL1823872 215810 40 None -4 5 Human 9.9 pKi = 9.9 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 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
16129706 215810 40 None -4 5 Human 9.6 pKi = 9.6 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm021093t
CHEMBL1823872 215810 40 None -4 5 Human 9.6 pKi = 9.6 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
CHEMBL3349606 218214 0 None -3 4 Human 9.5 pKi = 9.5 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
16129706 215810 40 None -4 5 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-somatostatin from human SSTR3 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR3 expressed in CHO-K1 cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2013.11.065
CHEMBL1823872 215810 40 None -4 5 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-somatostatin from human SSTR3 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR3 expressed in CHO-K1 cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2013.11.065
CHEMBL1823873 215811 9 None -1 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-somatostatin from human SSTR3 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR3 expressed in CHO-K1 cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2013.11.065
CHEMBL3349516 218196 0 None -7 4 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
CHEMBL3349517 218197 0 None -1 4 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
CHEMBL3349521 218200 0 None -5 4 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
CHEMBL3349605 218213 0 None -2 4 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
2070 7484 5 None 3467 4 Human 9.2 pKi = 9.2 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/ml200272z
9802572 7484 5 None 3467 4 Human 9.2 pKi = 9.2 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/ml200272z
CHEMBL2069499 7484 5 None 3467 4 Human 9.2 pKi = 9.2 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/ml200272z
11112736 23301 0 None 3090 3 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/ml500079u
CHEMBL1237140 23301 0 None 3090 3 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/ml500079u
CHEMBL1788167 23301 0 None 3090 3 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/ml500079u
2070 7484 5 None 3467 4 Human 9.2 pKi = 9.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/jm0108449
9802572 7484 5 None 3467 4 Human 9.2 pKi = 9.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/jm0108449
CHEMBL2069499 7484 5 None 3467 4 Human 9.2 pKi = 9.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/jm0108449
16129706 215810 40 None -4 5 Human 9.2 pKi = 9.2 Binding
Binding affinity towards Somatostatin receptor type 3 (hsst3)Binding affinity towards Somatostatin receptor type 3 (hsst3)
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm020424z
CHEMBL1823872 215810 40 None -4 5 Human 9.2 pKi = 9.2 Binding
Binding affinity towards Somatostatin receptor type 3 (hsst3)Binding affinity towards Somatostatin receptor type 3 (hsst3)
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm020424z
CHEMBL408362 219489 0 None -16 5 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human sst3 receptor expressed in CHO-K1 cellsBinding affinity towards human sst3 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
11112736 23301 0 None 3090 3 Human 9.1 pKi = 9.1 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL1237140 23301 0 None 3090 3 Human 9.1 pKi = 9.1 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL1788167 23301 0 None 3090 3 Human 9.1 pKi = 9.1 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
2018 9781 28 None -6 4 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
9941444 9781 28 None -6 4 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL3349607 9781 28 None -6 4 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
DB06663 9781 28 None -6 4 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL3349522 218201 0 None -5 4 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
CHEMBL3349601 218209 0 None -1 4 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
CHEMBL3349602 218210 0 None -1 5 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
90644992 118603 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 426 5 2 2 6.0 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc2ccccc2c1 10.1021/ml500079u
CHEMBL3287628 118603 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 426 5 2 2 6.0 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc2ccccc2c1 10.1021/ml500079u
73348312 96013 0 None 4897 2 Human 9.1 pKi = 9.1 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 410 3 3 2 6.2 CC1(C2CCCCC2)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL2367844 96013 0 None 4897 2 Human 9.1 pKi = 9.1 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 410 3 3 2 6.2 CC1(C2CCCCC2)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
91809303 132556 0 None -2 6 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 1659 28 18 16 3.8 CC(=O)N(CCC(=O)N[C@@H](CN[C@@H]1CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O)Cc1ccc(O)cc1)C[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 nan
CHEMBL3647702 132556 0 None -2 6 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 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
73348311 96007 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 454 10 3 2 7.8 CCCCCC1(CCCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL2367837 96007 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 454 10 3 2 7.8 CCCCCC1(CCCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
16129706 215810 40 None -4 5 Human 8.9 pKi = 8.9 Binding
Binding affinity towards somatostatin receptor type 3Binding affinity towards somatostatin receptor type 3
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm050376t
CHEMBL1823872 215810 40 None -4 5 Human 8.9 pKi = 8.9 Binding
Binding affinity towards somatostatin receptor type 3Binding affinity towards somatostatin receptor type 3
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
CHEMBL1794035 215716 0 None -4 5 Human 8.9 pKi = 8.9 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
CHEMBL442494 220692 0 None -4 5 Human 8.9 pKi = 8.9 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
122186640 129660 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 359 7 2 2 5.4 Cc1ccc(-c2c[nH]c(C3(NCCCc4ccccc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605798 129660 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 359 7 2 2 5.4 Cc1ccc(-c2c[nH]c(C3(NCCCc4ccccc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
91809276 132531 0 None -4 6 Human 8.8 pKi = 8.8 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 1620 27 18 16 4.3 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL3647677 132531 0 None -4 6 Human 8.8 pKi = 8.8 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 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
CHEMBL3349524 218202 0 None -2 4 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
CHEMBL3349599 218207 0 None -5 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
11069321 83620 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/ml200272z
CHEMBL2069500 83620 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human SST3 receptorBinding affinity to human SST3 receptor
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c([C@H]3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/ml200272z
44332931 11397 0 None 1047 2 Human 8.8 pKi = 8.8 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c(C3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/jm0108449
CHEMBL102892 11397 0 None 1047 2 Human 8.8 pKi = 8.8 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c(C3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/jm0108449
CHEMBL1201959 11397 0 None 1047 2 Human 8.8 pKi = 8.8 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c(C3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/jm0108449
CHEMBL3349603 218211 0 None -3 5 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
91809275 132530 0 None -89 6 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1603 27 18 17 3.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647676 132530 0 None -89 6 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 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
44397389 130822 0 None -58 5 Human 7.0 pKi = 7 Binding
Binding affinity against human sst3 receptor at 10 uMBinding affinity against human sst3 receptor at 10 uM
ChEMBL 460 9 2 6 5.2 NCCCCn1c(SCCc2c[nH]c3cc(F)ccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL363092 130822 0 None -58 5 Human 7.0 pKi = 7 Binding
Binding affinity against human sst3 receptor at 10 uMBinding affinity against human sst3 receptor at 10 uM
ChEMBL 460 9 2 6 5.2 NCCCCn1c(SCCc2c[nH]c3cc(F)ccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL2372961 217106 0 None -8 4 Human 7.0 pKi = 7 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
CHEMBL2369733 216440 0 None -5 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
CHEMBL2369759 216456 0 None -1 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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 218195 0 None -12 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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 218203 0 None -10 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
44377591 62407 0 None -4 4 Human 5.0 pKi = 5 Binding
Inhibitory constant on human somatostatin receptor type 3Inhibitory constant on human somatostatin receptor type 3
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 62407 0 None -4 4 Human 5.0 pKi = 5 Binding
Inhibitory constant on human somatostatin receptor type 3Inhibitory constant on human somatostatin receptor type 3
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
90644987 118596 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 397 8 2 3 4.5 CCN(CC)c1ccc(CN[C@H]2CCCC[C@H]2NC(=O)c2ccc(F)cc2)cc1 10.1021/ml500079u
CHEMBL3287619 118596 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 397 8 2 3 4.5 CCN(CC)c1ccc(CN[C@H]2CCCC[C@H]2NC(=O)c2ccc(F)cc2)cc1 10.1021/ml500079u
CHEMBL384607 219112 0 None -1 3 Human 7.0 pKi = 7.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
CHEMBL385745 219142 0 None 1 4 Human 7.0 pKi = 7.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
73346796 96008 0 None - 1 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-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 370 4 3 2 5.5 CCC1(CC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL2367838 96008 0 None - 1 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-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 370 4 3 2 5.5 CCC1(CC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
73355920 96009 0 None - 1 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-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 384 6 3 2 6.1 CCCCCC1N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL2367839 96009 0 None - 1 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-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 384 6 3 2 6.1 CCCCCC1N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL413171 219830 0 None 1 5 Human 7.0 pKi = 7.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
142471801 199078 0 None -616 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 494 9 2 5 5.3 COc1ccc2[nH]cc(Cc3nnc(Cc4cccc(C(F)(F)F)c4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
CHEMBL5206148 199078 0 None -616 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) 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
CHEMBL2311098 216284 0 None -8 5 Human 6.9 pKi = 6.9 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
CHEMBL2372956 217101 0 None -21 4 Human 5.9 pKi = 5.9 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
CHEMBL407195 219425 0 None -6 4 Human 6.9 pKi = 6.9 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
122186655 129675 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 339 5 2 3 4.2 Cc1ccc(-c2c[nH]c(C3(NCC4CCOCC4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605813 129675 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 339 5 2 3 4.2 Cc1ccc(-c2c[nH]c(C3(NCC4CCOCC4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
71458043 85678 0 None 1 5 Human 5.9 pKi = 5.9 Binding
Inhibitory constant on human somatostatin receptor type 3Inhibitory constant on human somatostatin receptor type 3
ChEMBL 494 10 3 5 4.3 CC(C)(C(=O)NCCc1c[nH]c2ccccc12)c1cn2cc(Cc3ccccc3)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
CHEMBL2112934 85678 0 None 1 5 Human 5.9 pKi = 5.9 Binding
Inhibitory constant on human somatostatin receptor type 3Inhibitory constant on human somatostatin receptor type 3
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
CHEMBL414598 219925 0 None -1 4 Human 6.9 pKi = 6.9 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
CHEMBL421362 220053 0 None -151 5 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
CHEMBL406738 219397 0 None -1 5 Human 6.9 pKi = 6.9 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
90644975 118617 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 384 5 2 3 4.7 O=C(O[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)c(F)c1 10.1021/ml500079u
CHEMBL3287646 118617 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 384 5 2 3 4.7 O=C(O[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)c(F)c1 10.1021/ml500079u
CHEMBL421362 220053 0 None -151 5 Human 6.9 pKi = 6.9 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst3) expressed in CHO-K1 cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst3) 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
44363816 46449 0 None -354 5 Human 5.9 pKi = 5.9 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 3 (hSSTR-3)In vitro binding affinity was evaluated against human Somatostatin receptor type 3 (hSSTR-3)
ChEMBL 589 14 3 5 5.0 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(CCCc2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL147499 46449 0 None -354 5 Human 5.9 pKi = 5.9 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 3 (hSSTR-3)In vitro binding affinity was evaluated against human Somatostatin receptor type 3 (hSSTR-3)
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
73354353 96011 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 416 2 3 2 5.4 c1ccc(-c2c[nH]c([C@@H]3Cc4c([nH]c5ccccc45)C4(Cc5ccccc5C4)N3)n2)cc1 10.1021/jm0108449
CHEMBL2367842 96011 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 416 2 3 2 5.4 c1ccc(-c2c[nH]c([C@@H]3Cc4c([nH]c5ccccc45)C4(Cc5ccccc5C4)N3)n2)cc1 10.1021/jm0108449
91809283 132538 0 None -165 6 Human 7.9 pKi = 7.9 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 1456 23 17 16 2.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3647684 132538 0 None -165 6 Human 7.9 pKi = 7.9 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 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
13690207 122160 0 None -30 5 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1039/C2MD20265D
CHEMBL3350037 122160 0 None -30 5 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst3 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
CHEMBL264539 217407 0 None -1 3 Human 5.9 pKi = 5.9 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
CHEMBL2369754 216451 0 None -15 5 Human 6.9 pKi = 6.9 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
122186653 129673 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 382 5 2 3 5.5 Cc1ccc(-c2c[nH]c(C3(NCc4ccc5ncccc5c4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605811 129673 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 382 5 2 3 5.5 Cc1ccc(-c2c[nH]c(C3(NCc4ccc5ncccc5c4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
44385757 68110 0 None 1 4 Human 5.9 pKi = 5.9 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 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 68110 0 None 1 4 Human 5.9 pKi = 5.9 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 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
91809288 132542 0 None -812 6 Human 6.8 pKi = 6.8 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 1472 23 17 16 1.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCC[S@@+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3647688 132542 0 None -812 6 Human 6.8 pKi = 6.8 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 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
CHEMBL2369758 216455 0 None -5 5 Human 6.8 pKi = 6.8 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
13690207 122160 0 None -30 5 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-somatostatin from human SSTR3 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR3 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 122160 0 None -30 5 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-somatostatin from human SSTR3 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR3 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
90644978 118620 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 365 5 3 2 4.6 O=C(Nc1ccc(F)cc1)[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12 10.1021/ml500079u
CHEMBL3287649 118620 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 365 5 3 2 4.6 O=C(Nc1ccc(F)cc1)[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12 10.1021/ml500079u
122186625 129645 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 342 5 3 2 4.6 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605783 129645 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 342 5 3 2 4.6 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CC3)n2)cc1 10.1016/j.bmcl.2015.06.087
90644994 118606 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 427 5 2 3 5.4 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc2ccccc2n1 10.1021/ml500079u
CHEMBL3287630 118606 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 427 5 2 3 5.4 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc2ccccc2n1 10.1021/ml500079u
CHEMBL275806 217602 0 None 1 4 Human 6.8 pKi = 6.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)O)NC1=O 10.1021/jm9806289
168275406 197086 0 None -1412 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 482 8 2 4 5.7 Fc1ccc2c(Cc3nnc(Cc4ccc(Cl)c(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5176083 197086 0 None -1412 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) 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
CHEMBL408787 219511 0 None -97 3 Human 5.8 pKi = 5.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
122186652 129672 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 407 6 2 2 6.6 Cc1ccc(-c2c[nH]c(C3(NCc4ccc(-c5ccccc5)cc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605810 129672 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 407 6 2 2 6.6 Cc1ccc(-c2c[nH]c(C3(NCc4ccc(-c5ccccc5)cc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL412859 219811 0 None -42 3 Human 5.8 pKi = 5.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
142471936 198274 0 None -2290 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 482 8 2 4 5.5 Fc1ccc2c(Cc3nnc(Cc4cccc(C(F)(F)F)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5193727 198274 0 None -2290 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) 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
CHEMBL385689 219138 0 None -2 4 Human 6.8 pKi = 6.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
90645007 118588 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 347 5 3 2 4.0 O=C(N[C@@H]1CCCC[C@@H]1NCc1cc2ccccc2[nH]1)c1ccccc1 10.1021/ml500079u
CHEMBL3287611 118588 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 347 5 3 2 4.0 O=C(N[C@@H]1CCCC[C@@H]1NCc1cc2ccccc2[nH]1)c1ccccc1 10.1021/ml500079u
11049745 114160 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 532 11 3 3 8.6 CCCCC1(CCCC)NC(c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccc(OCc3ccccc3)cc21 10.1021/jm0108449
CHEMBL317851 114160 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 532 11 3 3 8.6 CCCCC1(CCCC)NC(c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccc(OCc3ccccc3)cc21 10.1021/jm0108449
11705763 175094 0 None -446 5 Human 6.8 pKi = 6.8 Binding
Binding affinity against human sst3 receptor at 10 uMBinding affinity against human sst3 receptor at 10 uM
ChEMBL 484 10 2 7 5.4 Cc1cccc2c(C(=O)CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
CHEMBL434159 175094 0 None -446 5 Human 6.8 pKi = 6.8 Binding
Binding affinity against human sst3 receptor at 10 uMBinding affinity against human sst3 receptor at 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
10411795 137397 0 None 15 3 Human 6.8 pKi = 6.8 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 receptor expressed in CHO cells
ChEMBL 457 6 4 2 5.9 O=C(Nc1ccc(F)cc1F)N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1 10.1016/s0960-894x(01)00107-x
CHEMBL368176 137397 0 None 15 3 Human 6.8 pKi = 6.8 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 receptor expressed in CHO cells
ChEMBL 457 6 4 2 5.9 O=C(Nc1ccc(F)cc1F)N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1 10.1016/s0960-894x(01)00107-x
CHEMBL437057 220482 0 None 3 3 Human 6.8 pKi = 6.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
44377555 64305 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Inhibitory constant on human somatostatin receptor type 3Inhibitory constant on human somatostatin receptor type 3
ChEMBL 384 5 1 5 5.2 NCCCc1nc(-c2csc3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
CHEMBL166247 64305 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Inhibitory constant on human somatostatin receptor type 3Inhibitory constant on human somatostatin receptor type 3
ChEMBL 384 5 1 5 5.2 NCCCc1nc(-c2csc3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
90665458 116035 0 None -1 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 632 11 3 6 2.5 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
CHEMBL3218120 116035 0 None -1 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 632 11 3 6 2.5 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
CHEMBL414386 219908 0 None -2 4 Human 6.8 pKi = 6.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
142471832 197054 0 None -2454 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 471 8 3 4 5.1 Fc1ccc2c(Cc3nnc(Cc4c[nH]c5cc(F)ccc45)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5175637 197054 0 None -2454 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) 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
CHEMBL429166 220288 0 None -1 4 Human 6.8 pKi = 6.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
CHEMBL264028 217382 0 None 1 5 Human 7.8 pKi = 7.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
122186624 129644 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 344 5 3 2 4.9 Cc1ccc(-c2c[nH]c(C(C)(C)NCc3c[nH]c4ccccc34)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605782 129644 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 344 5 3 2 4.9 Cc1ccc(-c2c[nH]c(C(C)(C)NCc3c[nH]c4ccccc34)n2)cc1 10.1016/j.bmcl.2015.06.087
2054 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
71306 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL264186 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL3349523 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
DB04894 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL3349604 218212 0 None -50 5 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
CHEMBL408987 219519 0 None -1 5 Human 6.7 pKi = 6.7 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
90644998 118616 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 379 5 2 2 4.5 CN(Cc1c[nH]c2ccccc12)[C@H]1CCCC[C@H]1NC(=O)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287643 118616 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 379 5 2 2 4.5 CN(Cc1c[nH]c2ccccc12)[C@H]1CCCC[C@H]1NC(=O)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3349514 218194 0 None -10 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
CHEMBL3349600 218208 0 None -999 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
122186631 129651 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 374 5 3 2 5.3 Fc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605789 129651 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 374 5 3 2 5.3 Fc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
91809277 132532 0 None -6 6 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1457 23 16 14 3.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL3647678 132532 0 None -6 6 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 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
CHEMBL3349513 218193 0 None -5 4 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
73354355 96015 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 435 4 3 4 5.4 O=[N+]([O-])c1ccccc1C1N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL2367846 96015 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 435 4 3 4 5.4 O=[N+]([O-])c1ccccc1C1N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
10210016 67209 0 None 7 3 Human 6.7 pKi = 6.7 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 receptor expressed in CHO cells
ChEMBL 441 6 4 2 5.7 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(F)cc1F 10.1016/s0960-894x(01)00107-x
CHEMBL175197 67209 0 None 7 3 Human 6.7 pKi = 6.7 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 receptor expressed in CHO cells
ChEMBL 441 6 4 2 5.7 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(F)cc1F 10.1016/s0960-894x(01)00107-x
90644985 118594 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 356 6 2 3 3.7 COc1ccc(CN[C@H]2CCCC[C@H]2NC(=O)c2ccc(F)cc2)cc1 10.1021/ml500079u
CHEMBL3287617 118594 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 356 6 2 3 3.7 COc1ccc(CN[C@H]2CCCC[C@H]2NC(=O)c2ccc(F)cc2)cc1 10.1021/ml500079u
10179247 67238 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 receptor expressed in CHO cells
ChEMBL 402 5 3 3 5.4 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1 10.1016/s0960-894x(01)00107-x
CHEMBL175356 67238 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 receptor expressed in CHO cells
ChEMBL 402 5 3 3 5.4 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1 10.1016/s0960-894x(01)00107-x
CHEMBL2372962 217107 0 None -2 3 Human 6.7 pKi = 6.7 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
90665459 116036 0 None -4 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 646 11 3 6 2.9 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CCC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
CHEMBL3218121 116036 0 None -4 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 646 11 3 6 2.9 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CCC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
122186647 129667 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 349 5 2 2 5.1 Cc1ccc(-c2c[nH]c(C3(NCc4ccc(F)cc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605805 129667 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 349 5 2 2 5.1 Cc1ccc(-c2c[nH]c(C3(NCc4ccc(F)cc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL2369760 216457 0 None 13 5 Human 7.6 pKi = 7.6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
CHEMBL2372963 217108 0 None -8 3 Human 6.6 pKi = 6.6 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
142471730 197164 0 None -2951 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 464 8 2 4 5.3 FC(F)(F)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5177487 197164 0 None -2951 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 464 8 2 4 5.3 FC(F)(F)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
90645000 118612 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 369 5 3 2 3.9 O=C(N[C@H]1CCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)c(F)c1 10.1021/ml500079u
CHEMBL3287636 118612 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 369 5 3 2 3.9 O=C(N[C@H]1CCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)c(F)c1 10.1021/ml500079u
3156873 118614 9 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 311 6 3 2 2.8 O=C(NCCNCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287639 118614 9 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 311 6 3 2 2.8 O=C(NCCNCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
90645014 118610 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 351 5 3 2 3.7 O=C(N[C@H]1CCC[C@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287634 118610 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 351 5 3 2 3.7 O=C(N[C@H]1CCC[C@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
122186635 129655 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 371 5 3 3 4.8 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5cccnc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605793 129655 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 371 5 3 3 4.8 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5cccnc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
122186636 129656 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 400 6 3 3 5.4 COc1cccc2c(CNC3(c4nc(-c5ccc(C)cc5)c[nH]4)CCCC3)c[nH]c12 10.1016/j.bmcl.2015.06.087
CHEMBL3605794 129656 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 400 6 3 3 5.4 COc1cccc2c(CNC3(c4nc(-c5ccc(C)cc5)c[nH]4)CCCC3)c[nH]c12 10.1016/j.bmcl.2015.06.087
90644980 118623 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 584 17 5 8 2.8 CCCCC(NC(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CCCCN)C(=O)OC 10.1021/ml500079u
CHEMBL3287652 118623 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 584 17 5 8 2.8 CCCCC(NC(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CCCCN)C(=O)OC 10.1021/ml500079u
44385591 138165 0 None 38 2 Human 6.6 pKi = 6.6 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 receptor expressed in CHO cells
ChEMBL 488 7 3 2 6.2 O=C(Cc1cccc(C(F)(F)F)c1)N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1 10.1016/s0960-894x(01)00107-x
CHEMBL368993 138165 0 None 38 2 Human 6.6 pKi = 6.6 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 receptor expressed in CHO cells
ChEMBL 488 7 3 2 6.2 O=C(Cc1cccc(C(F)(F)F)c1)N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1 10.1016/s0960-894x(01)00107-x
90665460 116037 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 793 13 3 7 3.9 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
CHEMBL3218122 116037 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst3 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
CHEMBL410181 219584 0 None 1 5 Human 6.6 pKi = 6.6 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
90644977 118619 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 410 5 2 3 5.8 O=C(Nc1ccc(F)cc1)O[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1 10.1021/ml500079u
CHEMBL3287648 118619 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 410 5 2 3 5.8 O=C(Nc1ccc(F)cc1)O[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1 10.1021/ml500079u
CHEMBL3349520 218199 0 None -1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
44385652 67166 0 None 6 5 Human 6.6 pKi = 6.6 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 receptor expressed in CHO cells
ChEMBL 405 6 4 2 5.5 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccccc1 10.1016/s0960-894x(01)00107-x
CHEMBL174872 67166 0 None 6 5 Human 6.6 pKi = 6.6 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 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
10248767 63966 0 None -5 4 Human 5.6 pKi = 5.6 Binding
Inhibitory constant on human somatostatin receptor type 3Inhibitory constant on human somatostatin receptor type 3
ChEMBL 373 6 1 6 3.9 NCCCc1nc(-c2cccc([N+](=O)[O-])c2)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
CHEMBL164964 63966 0 None -5 4 Human 5.6 pKi = 5.6 Binding
Inhibitory constant on human somatostatin receptor type 3Inhibitory constant on human somatostatin receptor type 3
ChEMBL 373 6 1 6 3.9 NCCCc1nc(-c2cccc([N+](=O)[O-])c2)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
CHEMBL2370168 216586 0 None -58 5 Human 6.6 pKi = 6.6 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst3) expressed in CHO-K1 cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst3) 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
9827283 85363 0 None -56 4 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human sst3 receptor expressed in CHO-K1 cellsBinding affinity towards human sst3 receptor expressed in CHO-K1 cells
ChEMBL 499 9 4 3 4.1 NCCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/jm980194h
CHEMBL2112223 85363 0 None -56 4 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human sst3 receptor expressed in CHO-K1 cellsBinding affinity towards human sst3 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
122186633 129653 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 384 5 2 3 5.4 Cc1ccc(-c2c[nH]c(C3(NCc4cn(C)c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605791 129653 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 384 5 2 3 5.4 Cc1ccc(-c2c[nH]c(C3(NCc4cn(C)c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
13690207 122160 0 None -30 5 Human 7.6 pKi = 7.6 Binding
Binding affinity towards somatostatin receptor type 3Binding affinity towards somatostatin receptor type 3
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 122160 0 None -30 5 Human 7.6 pKi = 7.6 Binding
Binding affinity towards somatostatin receptor type 3Binding affinity towards somatostatin receptor type 3
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
122186643 129663 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 337 5 2 2 4.7 Cc1ccc(-c2c[nH]c(C3(NCCC(F)(F)F)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605801 129663 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 337 5 2 2 4.7 Cc1ccc(-c2c[nH]c(C3(NCCC(F)(F)F)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
9851998 31357 0 None -5248 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to hsst3 was determinedBinding affinity to hsst3 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 31357 0 None -5248 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to hsst3 was determinedBinding affinity to hsst3 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
CHEMBL407496 219444 0 None -8 5 Human 6.6 pKi = 6.6 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
122186654 129674 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 337 5 2 2 5.3 Cc1ccc(-c2c[nH]c(C3(NCC4CCCCC4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605812 129674 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 337 5 2 2 5.3 Cc1ccc(-c2c[nH]c(C3(NCC4CCCCC4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
91809286 132541 0 None -177 6 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1489 23 16 15 2.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCS(=O)(=O)C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL3647687 132541 0 None -177 6 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 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
90665463 116039 0 None 4 5 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 882 28 3 9 4.5 COC(=O)CCN(Cc1ccccc1)C(=O)CCN(C[C@@H](C)O)C(=O)CCN(CCCCN)C(=O)CCN(CCc1c[nH]c2ccccc12)C(=O)CCN(Cc1ccccc1)C(C)=O 10.1039/C2MD20265D
CHEMBL3218124 116039 0 None 4 5 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst3 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
CHEMBL415201 219959 0 None -7 4 Human 6.6 pKi = 6.6 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
142471848 198046 0 None -2754 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 8 2 4 5.2 Fc1ccc2c(Cc3nnc(Cc4cccc(Br)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5190457 198046 0 None -2754 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) 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
73352847 96006 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 482 12 3 2 8.6 CCCCCCC1(CCCCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL2367836 96006 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 482 12 3 2 8.6 CCCCCCC1(CCCCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
9852911 106159 0 None -18 6 Human 5.6 pKi = 5.6 Binding
Binding affinity for human receptor subtype hSSTR3.Binding affinity for human receptor subtype hSSTR3.
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL282618 106159 0 None -18 6 Human 5.6 pKi = 5.6 Binding
Binding affinity for human receptor subtype hSSTR3.Binding affinity for human receptor subtype hSSTR3.
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
CHEMBL439005 220596 0 None -5 4 Human 6.5 pKi = 6.5 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
90644999 118622 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 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
CHEMBL3287651 118622 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 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
44308969 211143 0 None -1862 5 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human sst3 receptor expressed in CHO-K1 cellsBinding affinity towards human sst3 receptor expressed in CHO-K1 cells
ChEMBL 539 7 4 3 4.7 NC[C@@H]1CCC[C@H](CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm980194h
CHEMBL71723 211143 0 None -1862 5 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human sst3 receptor expressed in CHO-K1 cellsBinding affinity towards human sst3 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
90644993 118604 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 444 5 2 2 6.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc2cc(F)ccc2c1 10.1021/ml500079u
CHEMBL3287629 118604 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 444 5 2 2 6.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc2cc(F)ccc2c1 10.1021/ml500079u
122186627 129647 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 370 5 3 2 5.4 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605785 129647 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 370 5 3 2 5.4 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
11112736 23301 0 None 3090 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL1237140 23301 0 None 3090 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL1788167 23301 0 None 3090 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
11048825 115833 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 460 8 3 2 7.7 CCCCC1(CCCC)NC(c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccc(Cl)cc21 10.1021/jm0108449
CHEMBL321282 115833 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 460 8 3 2 7.7 CCCCC1(CCCC)NC(c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccc(Cl)cc21 10.1021/jm0108449
90644996 118608 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 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
CHEMBL3287632 118608 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 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
90644981 118590 0 None 81 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 365 5 3 2 4.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287613 118590 0 None 81 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 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
90644997 118611 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 369 5 3 2 3.9 O=C(N[C@@H]1CCC[C@H]1NCc1c[nH]c2ccccc12)c1ccc(F)c(F)c1 10.1021/ml500079u
CHEMBL3287635 118611 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 369 5 3 2 3.9 O=C(N[C@@H]1CCC[C@H]1NCc1c[nH]c2ccccc12)c1ccc(F)c(F)c1 10.1021/ml500079u
91809287 167037 0 None -616 6 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1472 23 17 16 1.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCC[S@+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL4110066 167037 0 None -616 6 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1472 23 17 16 1.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCC[S@+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
10325243 107271 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Binding affinity for human receptor subtype hSSTR3.Binding affinity for human receptor subtype hSSTR3.
ChEMBL 549 17 1 7 5.3 CO[C@@H]1O[C@H](COCCCCCN)[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL29102 107271 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Binding affinity for human receptor subtype hSSTR3.Binding affinity for human receptor subtype hSSTR3.
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
15965425 8987 7 None -3090 5 Human 7.5 pKi = 7.5 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 645 11 5 7 4.3 NCCCC[C@@H](C(=O)OC(C)(C)C)NC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01029
2046 8987 7 None -3090 5 Human 7.5 pKi = 7.5 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 645 11 5 7 4.3 NCCCC[C@@H](C(=O)OC(C)(C)C)NC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01029
CHEMBL99895 8987 7 None -3090 5 Human 7.5 pKi = 7.5 Binding
Binding affinity to human somatostatin receptor type 3Binding affinity to human somatostatin receptor type 3
ChEMBL 645 11 5 7 4.3 NCCCC[C@@H](C(=O)OC(C)(C)C)NC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01029
15965425 8987 7 None -3090 5 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Somatostatin receptor type 3 (hsst3)Binding affinity towards Somatostatin receptor type 3 (hsst3)
ChEMBL 645 11 5 7 4.3 NCCCC[C@@H](C(=O)OC(C)(C)C)NC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm020424z
2046 8987 7 None -3090 5 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Somatostatin receptor type 3 (hsst3)Binding affinity towards Somatostatin receptor type 3 (hsst3)
ChEMBL 645 11 5 7 4.3 NCCCC[C@@H](C(=O)OC(C)(C)C)NC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm020424z
CHEMBL99895 8987 7 None -3090 5 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Somatostatin receptor type 3 (hsst3)Binding affinity towards Somatostatin receptor type 3 (hsst3)
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
122186632 129652 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 432 6 3 2 6.8 c1ccc(-c2ccc(-c3c[nH]c(C4(NCc5c[nH]c6ccccc56)CCCC4)n3)cc2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605790 129652 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 432 6 3 2 6.8 c1ccc(-c2ccc(-c3c[nH]c(C4(NCc5c[nH]c6ccccc56)CCCC4)n3)cc2)cc1 10.1016/j.bmcl.2015.06.087
2051 10349 24 None -218 9 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
5311430 10349 24 None -218 9 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL311695 10349 24 None -218 9 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
90665462 116007 0 None 4 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 867 27 3 9 4.1 COC(=O)CCN(Cc1ccccc1)C(=O)CCN(C[C@@H](C)O)C(=O)CCN(CCCCN)C(=O)CN(CCc1c[nH]c2ccccc12)C(=O)CCN(Cc1ccccc1)C(C)=O 10.1039/C2MD20265D
CHEMBL3217760 116007 0 None 4 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 867 27 3 9 4.1 COC(=O)CCN(Cc1ccccc1)C(=O)CCN(C[C@@H](C)O)C(=O)CCN(CCCCN)C(=O)CN(CCc1c[nH]c2ccccc12)C(=O)CCN(Cc1ccccc1)C(C)=O 10.1039/C2MD20265D
71461645 85679 0 None -3 4 Human 5.5 pKi = 5.5 Binding
Inhibitory constant on human somatostatin receptor type 3Inhibitory constant on human somatostatin receptor type 3
ChEMBL 367 5 2 4 4.4 NCCCc1nc(-c2c[nH]c3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
CHEMBL2112935 85679 0 None -3 4 Human 5.5 pKi = 5.5 Binding
Inhibitory constant on human somatostatin receptor type 3Inhibitory constant on human somatostatin receptor type 3
ChEMBL 367 5 2 4 4.4 NCCCc1nc(-c2c[nH]c3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
CHEMBL2369753 216450 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
122186644 129664 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 361 6 2 3 5.0 COc1ccc(CNC2(c3nc(-c4ccc(C)cc4)c[nH]3)CCCC2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605802 129664 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 361 6 2 3 5.0 COc1ccc(CNC2(c3nc(-c4ccc(C)cc4)c[nH]3)CCCC2)cc1 10.1016/j.bmcl.2015.06.087
122186645 129665 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 365 5 2 2 5.6 Cc1ccc(-c2c[nH]c(C3(NCc4ccc(Cl)cc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605803 129665 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 365 5 2 2 5.6 Cc1ccc(-c2c[nH]c(C3(NCc4ccc(Cl)cc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
90645008 118589 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 347 5 3 2 4.0 O=C(N[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccccc1 10.1021/ml500079u
CHEMBL3287612 118589 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 347 5 3 2 4.0 O=C(N[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccccc1 10.1021/ml500079u
73355921 96012 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 391 3 3 3 4.9 c1ccc(-c2c[nH]c([C@@H]3Cc4c([nH]c5ccccc45)C(c4ccncc4)N3)n2)cc1 10.1021/jm0108449
CHEMBL2367843 96012 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 391 3 3 3 4.9 c1ccc(-c2c[nH]c([C@@H]3Cc4c([nH]c5ccccc45)C(c4ccncc4)N3)n2)cc1 10.1021/jm0108449
73354354 96014 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 433 4 3 3 5.6 CN(C)c1ccc(C2N[C@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)cc1 10.1021/jm0108449
CHEMBL2367845 96014 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 433 4 3 3 5.6 CN(C)c1ccc(C2N[C@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)cc1 10.1021/jm0108449
CHEMBL2369750 216447 0 None -9 5 Human 6.5 pKi = 6.5 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
122186646 129666 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 399 5 2 2 6.0 Cc1ccc(-c2c[nH]c(C3(NCc4ccc(C(F)(F)F)cc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605804 129666 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 399 5 2 2 6.0 Cc1ccc(-c2c[nH]c(C3(NCc4ccc(C(F)(F)F)cc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
9985523 105937 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Binding affinity for human receptor subtype hSSTR3.Binding affinity for human receptor subtype hSSTR3.
ChEMBL 572 17 2 6 6.2 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)C[C@@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL281200 105937 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Binding affinity for human receptor subtype hSSTR3.Binding affinity for human receptor subtype hSSTR3.
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
10770814 107569 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Binding affinity for human receptor subtype hSSTR3.Binding affinity for human receptor subtype hSSTR3.
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL29311 107569 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Binding affinity for human receptor subtype hSSTR3.Binding affinity for human receptor subtype hSSTR3.
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
122186656 129676 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 335 5 2 4 3.7 Cc1ccc(-c2c[nH]c(C3(NCc4cnn(C)c4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605814 129676 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 335 5 2 4 3.7 Cc1ccc(-c2c[nH]c(C3(NCc4cnn(C)c4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
122186642 129662 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 325 5 2 2 5.2 Cc1ccc(-c2c[nH]c(C3(NCCC(C)(C)C)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605800 129662 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 325 5 2 2 5.2 Cc1ccc(-c2c[nH]c(C3(NCCC(C)(C)C)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
10094509 137464 0 None 44 5 Human 7.4 pKi = 7.4 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 receptor expressed in CHO cells
ChEMBL 435 7 4 3 5.5 COc1ccc(C(=N)N[C@H](Cc2c[nH]c3ccccc23)c2nc(-c3ccccc3)c[nH]2)cc1 10.1016/s0960-894x(01)00107-x
CHEMBL368334 137464 0 None 44 5 Human 7.4 pKi = 7.4 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 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
44308836 109568 0 None -912 5 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human sst3 receptor expressed in CHO-K1 cellsBinding affinity towards human sst3 receptor expressed in CHO-K1 cells
ChEMBL 539 7 4 3 4.7 NCC1CCCC(CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm980194h
CHEMBL305279 109568 0 None -912 5 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human sst3 receptor expressed in CHO-K1 cellsBinding affinity towards human sst3 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
44309052 210726 0 None -186 5 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human sst3 receptor expressed in CHO-K1 cellsBinding affinity towards human sst3 receptor expressed in CHO-K1 cells
ChEMBL 539 7 4 3 4.7 NC[C@H]1CCC[C@@H](CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm980194h
CHEMBL69303 210726 0 None -186 5 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human sst3 receptor expressed in CHO-K1 cellsBinding affinity towards human sst3 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
122186639 129659 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 345 6 2 2 5.0 Cc1ccc(-c2c[nH]c(C3(NCCc4ccccc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605797 129659 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 345 6 2 2 5.0 Cc1ccc(-c2c[nH]c(C3(NCCc4ccccc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
90644984 118593 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 344 5 2 2 3.8 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(F)cc1)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287616 118593 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 344 5 2 2 3.8 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(F)cc1)c1ccc(F)cc1 10.1021/ml500079u
10096510 64202 0 None -10 4 Human 5.4 pKi = 5.4 Binding
Inhibitory constant on human somatostatin receptor type 3Inhibitory constant on human somatostatin receptor type 3
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 64202 0 None -10 4 Human 5.4 pKi = 5.4 Binding
Inhibitory constant on human somatostatin receptor type 3Inhibitory constant on human somatostatin receptor type 3
ChEMBL 475 7 2 6 5.2 CC(C)(C(=O)NC1CCCCC1)c1cn2cc(-c3csc4ccccc34)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
CHEMBL2372960 217105 0 None -10 4 Human 6.4 pKi = 6.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
44354386 29381 0 None -30 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to hsst3 was determinedBinding affinity to hsst3 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 29381 0 None -30 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to hsst3 was determinedBinding affinity to hsst3 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
CHEMBL414116 219890 0 None -1 4 Human 6.4 pKi = 6.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
CHEMBL408347 219486 0 None -3 4 Human 7.4 pKi = 7.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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 216446 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
9803492 11549 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 443 8 2 3 7.8 CCCCC1(CCCC)N[C@@H](c2nc(-c3ccccc3)cs2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL103987 11549 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 443 8 2 3 7.8 CCCCC1(CCCC)N[C@@H](c2nc(-c3ccccc3)cs2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL1202952 11549 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 443 8 2 3 7.8 CCCCC1(CCCC)N[C@@H](c2nc(-c3ccccc3)cs2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL406491 219390 0 None -10 4 Human 6.4 pKi = 6.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
CHEMBL438281 220542 0 None -2 4 Human 6.4 pKi = 6.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
90644979 118621 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 365 5 3 2 4.6 O=C(Nc1ccc(F)cc1)[C@@H]1CCCC[C@H]1NCc1c[nH]c2ccccc12 10.1021/ml500079u
CHEMBL3287650 118621 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 365 5 3 2 4.6 O=C(Nc1ccc(F)cc1)[C@@H]1CCCC[C@H]1NCc1c[nH]c2ccccc12 10.1021/ml500079u
CHEMBL2369752 216449 0 None -7 5 Human 6.4 pKi = 6.4 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
CHEMBL411556 219665 0 None -6 4 Human 6.4 pKi = 6.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
91809285 132540 0 None -30 6 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 1880 34 19 19 5.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](CCCCNC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647686 132540 0 None -30 6 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 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
90645013 118609 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 351 5 3 2 3.7 O=C(N[C@@H]1CCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287633 118609 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 351 5 3 2 3.7 O=C(N[C@@H]1CCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3098601 217797 0 None -21 5 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-somatostatin from human SSTR3 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR3 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
90644991 118602 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 412 5 2 2 5.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc(F)c(F)c1 10.1021/ml500079u
CHEMBL3287627 118602 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 412 5 2 2 5.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc(F)c(F)c1 10.1021/ml500079u
122186637 129657 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 370 5 3 2 5.4 Cc1ccc(-c2c[nH]c(C3(NCc4cc5ccccc5[nH]4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605795 129657 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 370 5 3 2 5.4 Cc1ccc(-c2c[nH]c(C3(NCc4cc5ccccc5[nH]4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL2371893 216926 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
44385508 136866 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 receptor expressed in CHO cells
ChEMBL 401 5 4 2 4.9 CC(C)(C)NC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1 10.1016/s0960-894x(01)00107-x
CHEMBL367716 136866 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 receptor expressed in CHO cells
ChEMBL 401 5 4 2 4.9 CC(C)(C)NC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1 10.1016/s0960-894x(01)00107-x
142471891 197374 0 None -2884 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 430 8 2 4 5.0 Clc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5180551 197374 0 None -2884 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) 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
44397706 73965 0 None -22 5 Human 7.4 pKi = 7.4 Binding
Binding affinity against human sst3 receptor at 10 uMBinding affinity against human sst3 receptor at 10 uM
ChEMBL 456 9 2 6 5.4 Cc1cccc2c(CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
CHEMBL187768 73965 0 None -22 5 Human 7.4 pKi = 7.4 Binding
Binding affinity against human sst3 receptor at 10 uMBinding affinity against human sst3 receptor at 10 uM
ChEMBL 456 9 2 6 5.4 Cc1cccc2c(CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
44385504 67822 0 None 2 5 Human 6.4 pKi = 6.4 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 receptor expressed in CHO cells
ChEMBL 489 7 4 3 6.4 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(OC(F)(F)F)cc1 10.1016/s0960-894x(01)00107-x
CHEMBL176313 67822 0 None 2 5 Human 6.4 pKi = 6.4 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 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
90644995 118607 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 426 5 2 2 6.0 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1cccc2ccccc12 10.1021/ml500079u
CHEMBL3287631 118607 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 426 5 2 2 6.0 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1cccc2ccccc12 10.1021/ml500079u
CHEMBL2370167 216585 0 None -190 5 Human 6.4 pKi = 6.4 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst3) expressed in CHO-K1 cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst3) 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
9803491 116210 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 443 8 2 3 7.8 CCCCC1(CCCC)N[C@@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1sc1ccccc21 10.1021/jm0108449
CHEMBL322012 116210 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 443 8 2 3 7.8 CCCCC1(CCCC)N[C@@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1sc1ccccc21 10.1021/jm0108449
168288485 198510 0 None -8709 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 430 8 2 4 5.0 Clc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5197201 198510 0 None -8709 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) 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
CHEMBL2369756 216453 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
90665461 116038 0 None -2 5 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 807 13 3 7 4.3 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CCC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
CHEMBL3218123 116038 0 None -2 5 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-somatostatin from human sst3 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst3 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
90645012 118601 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 406 6 2 3 4.8 COc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NCc2ccc(Cl)c(Cl)c2)cc1 10.1021/ml500079u
CHEMBL3287626 118601 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 406 6 2 3 4.8 COc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NCc2ccc(Cl)c(Cl)c2)cc1 10.1021/ml500079u
CHEMBL413709 219862 0 None -2 3 Human 6.3 pKi = 6.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
CHEMBL406152 219375 0 None -6 4 Human 6.3 pKi = 6.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
13690207 122160 0 None -30 5 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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 122160 0 None -30 5 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
122186628 129648 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 384 5 3 2 5.8 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605786 129648 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 384 5 3 2 5.8 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
122186630 129650 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 356 5 3 2 5.1 c1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605788 129650 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 356 5 3 2 5.1 c1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL446077 220722 0 None -9 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned sst3 receptorBinding affinity to human cloned sst3 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
44386389 136861 0 None 4 5 Human 6.3 pKi = 6.3 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 receptor expressed in CHO cells
ChEMBL 473 6 4 2 6.5 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(C(F)(F)F)cc1 10.1016/s0960-894x(01)00107-x
CHEMBL367699 136861 0 None 4 5 Human 6.3 pKi = 6.3 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 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
122186626 129646 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 356 5 3 2 5.0 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605784 129646 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 356 5 3 2 5.0 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL439136 220606 0 None -1 4 Human 7.3 pKi = 7.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
122186641 129661 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 283 5 2 2 4.2 CCCNC1(c2nc(-c3ccc(C)cc3)c[nH]2)CCCC1 10.1016/j.bmcl.2015.06.087
CHEMBL3605799 129661 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 283 5 2 2 4.2 CCCNC1(c2nc(-c3ccc(C)cc3)c[nH]2)CCCC1 10.1016/j.bmcl.2015.06.087
44354398 122280 0 None -346 3 Human 5.3 pKi = 5.3 Binding
Binding affinity to hsst3 was determinedBinding affinity to hsst3 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 122280 0 None -346 3 Human 5.3 pKi = 5.3 Binding
Binding affinity to hsst3 was determinedBinding affinity to hsst3 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
CHEMBL385746 219143 0 None -3 4 Human 7.3 pKi = 7.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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 216454 0 None -21 5 Human 6.3 pKi = 6.3 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
168279197 197711 0 None -8912 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5185547 197711 0 None -8912 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) 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
73351385 96005 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 502 9 3 2 8.7 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c(-c3ccccc3)[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL2367835 96005 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 502 9 3 2 8.7 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c(-c3ccccc3)[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL2372964 217109 0 None -4 4 Human 6.3 pKi = 6.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
122186649 129669 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 332 5 2 3 4.3 Cc1ccc(-c2c[nH]c(C3(NCc4ccncc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605807 129669 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 332 5 2 3 4.3 Cc1ccc(-c2c[nH]c(C3(NCc4ccncc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL2372959 217104 0 None -2 5 Human 6.3 pKi = 6.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
9848232 108930 0 None -9 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human sst3 receptor expressed in CHO-K1 cellsBinding affinity towards human sst3 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 108930 0 None -9 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human sst3 receptor expressed in CHO-K1 cellsBinding affinity towards human sst3 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
CHEMBL437448 220498 0 None -3 5 Human 7.2 pKi = 7.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
CHEMBL2369751 216448 0 None -6 5 Human 6.2 pKi = 6.2 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
CHEMBL2372957 217102 0 None -3 4 Human 7.2 pKi = 7.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
90645005 118615 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 388 5 2 2 6.0 O=C(Nc1ccccc1NCc1ccc(Cl)c(Cl)c1)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287642 118615 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 388 5 2 2 6.0 O=C(Nc1ccccc1NCc1ccc(Cl)c(Cl)c1)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL2369761 216458 0 None -5 5 Human 6.2 pKi = 6.2 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
90644982 118591 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 394 5 2 2 5.0 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287614 118591 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 394 5 2 2 5.0 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc(F)cc1 10.1021/ml500079u
10917657 66841 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 468 10 3 2 8.1 CCCCCC1(CCCCC)NC(c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccc(C)cc21 10.1021/jm0108449
CHEMBL173778 66841 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 468 10 3 2 8.1 CCCCCC1(CCCCC)NC(c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccc(C)cc21 10.1021/jm0108449
122186629 129649 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 385 5 4 3 4.2 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCNCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605787 129649 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 385 5 4 3 4.2 Cc1ccc(-c2c[nH]c(C3(NCc4c[nH]c5ccccc45)CCNCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
9802240 96010 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 420 4 3 3 5.5 COc1ccc(C2N[C@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)cc1 10.1021/jm0108449
CHEMBL2367841 96010 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 420 4 3 3 5.5 COc1ccc(C2N[C@H](c3nc(-c4ccccc4)c[nH]3)Cc3c2[nH]c2ccccc32)cc1 10.1021/jm0108449
10580397 106091 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Binding affinity for human receptor subtype hSSTR3.Binding affinity for human receptor subtype hSSTR3.
ChEMBL 677 20 3 7 6.9 NCCCCCNC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL282129 106091 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Binding affinity for human receptor subtype hSSTR3.Binding affinity for human receptor subtype hSSTR3.
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
10554930 106968 0 None -2 5 Human 5.2 pKi = 5.2 Binding
Binding affinity for human receptor subtype hSSTR3.Binding affinity for human receptor subtype hSSTR3.
ChEMBL 562 17 3 7 4.9 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)C[C@@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL28824 106968 0 None -2 5 Human 5.2 pKi = 5.2 Binding
Binding affinity for human receptor subtype hSSTR3.Binding affinity for human receptor subtype hSSTR3.
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
CHEMBL1201185 215380 28 None -125 4 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
10699714 106193 0 None -3 5 Human 5.2 pKi = 5.2 Binding
Binding affinity for human receptor subtype hSSTR3.Binding affinity for human receptor subtype hSSTR3.
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL282803 106193 0 None -3 5 Human 5.2 pKi = 5.2 Binding
Binding affinity for human receptor subtype hSSTR3.Binding affinity for human receptor subtype hSSTR3.
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
90644983 118592 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 340 5 2 2 4.0 Cc1ccc(CN[C@H]2CCCC[C@H]2NC(=O)c2ccc(F)cc2)cc1 10.1021/ml500079u
CHEMBL3287615 118592 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 340 5 2 2 4.0 Cc1ccc(CN[C@H]2CCCC[C@H]2NC(=O)c2ccc(F)cc2)cc1 10.1021/ml500079u
90644989 118598 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 354 7 2 2 4.1 O=C(N[C@@H]1CCCC[C@@H]1NCCCc1ccccc1)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287621 118598 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 354 7 2 2 4.1 O=C(N[C@@H]1CCCC[C@@H]1NCCCc1ccccc1)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL2369755 216452 0 None -10 5 Human 7.2 pKi = 7.2 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
56945132 178199 0 None -346 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Tyr-SRIF from SST3 receptor (unknown origin) after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from SST3 receptor (unknown origin) after 90 mins by gamma counting method
ChEMBL 478 9 2 4 5.8 Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl 10.1039/C8MD00388B
CHEMBL4462793 178199 0 None -346 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Tyr-SRIF from SST3 receptor (unknown origin) after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from SST3 receptor (unknown origin) after 90 mins by gamma counting method
ChEMBL 478 9 2 4 5.8 Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl 10.1039/C8MD00388B
CHEMBL2369734 216441 0 None 2 5 Human 7.2 pKi = 7.2 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
142471737 197083 0 None -169 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 1 5 5.8 Cn1cc(CCc2nnc(Cc3ccc(Cl)c(Cl)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
CHEMBL5176020 197083 0 None -169 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST3 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 1 5 5.8 Cn1cc(CCc2nnc(Cc3ccc(Cl)c(Cl)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
91809284 132539 0 None -36 6 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1896 34 20 20 5.5 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](CCCCNC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3647685 132539 0 None -36 6 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 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
CHEMBL3349518 218198 0 None -12 4 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 3 (sst3) 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
44385712 67118 0 None 1 4 Human 6.2 pKi = 6.2 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 receptor expressed in CHO cells
ChEMBL 343 5 4 2 4.4 CC(=N)N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1 10.1016/s0960-894x(01)00107-x
CHEMBL174490 67118 0 None 1 4 Human 6.2 pKi = 6.2 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 receptor expressed in CHO cells
ChEMBL 343 5 4 2 4.4 CC(=N)N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1 10.1016/s0960-894x(01)00107-x
CHEMBL2372958 217103 0 None -1 3 Human 6.2 pKi = 6.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
10960879 85453 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 425 2 3 3 4.3 CC(=O)N1CCC2(CC1)N[C@@H](c1nc(-c3ccccc3)c[nH]1)Cc1c2[nH]c2ccccc12 10.1021/jm0108449
CHEMBL2112415 85453 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 425 2 3 3 4.3 CC(=O)N1CCC2(CC1)N[C@@H](c1nc(-c3ccccc3)c[nH]1)Cc1c2[nH]c2ccccc12 10.1021/jm0108449
122186648 129668 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 349 5 2 2 5.1 Cc1ccc(-c2c[nH]c(C3(NCc4cccc(F)c4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605806 129668 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 349 5 2 2 5.1 Cc1ccc(-c2c[nH]c(C3(NCc4cccc(F)c4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
122186634 129654 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 384 6 3 2 5.5 Cc1ccc(-c2c[nH]c(C3(NCCc4c[nH]c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605792 129654 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 384 6 3 2 5.5 Cc1ccc(-c2c[nH]c(C3(NCCc4c[nH]c5ccccc45)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
11025614 114153 0 None - 1 Human 6.1 pKi = 6.1 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 392 3 2 2 6.8 c1ccc(-c2c[nH]c(-c3cc4c([nH]c5ccccc54)c(C4CCCCC4)n3)n2)cc1 10.1021/jm0108449
CHEMBL317808 114153 0 None - 1 Human 6.1 pKi = 6.1 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 392 3 2 2 6.8 c1ccc(-c2c[nH]c(-c3cc4c([nH]c5ccccc54)c(C4CCCCC4)n3)n2)cc1 10.1021/jm0108449
90644990 118599 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 320 5 2 2 3.9 CC(C)(C)CCN[C@H]1CCCC[C@H]1NC(=O)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287622 118599 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 320 5 2 2 3.9 CC(C)(C)CCN[C@H]1CCCC[C@H]1NC(=O)c1ccc(F)cc1 10.1021/ml500079u
10166743 130724 0 None 8 5 Human 7.1 pKi = 7.1 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 receptor expressed in CHO cells
ChEMBL 439 6 4 2 6.1 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(Cl)cc1 10.1016/s0960-894x(01)00107-x
CHEMBL362859 130724 0 None 8 5 Human 7.1 pKi = 7.1 Binding
Inhibition of human sst3 receptor expressed in CHO cellsInhibition of human sst3 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
CHEMBL2370166 216584 0 None -38 5 Human 6.1 pKi = 6.1 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst3) expressed in CHO-K1 cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst3) 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
44387399 175796 0 None -2 3 Human 6.1 pKi = 6.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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 175796 0 None -2 3 Human 6.1 pKi = 6.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
122186651 129671 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 389 6 2 4 4.7 COC(=O)c1ccc(CNC2(c3nc(-c4ccc(C)cc4)c[nH]3)CCCC2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605809 129671 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 389 6 2 4 4.7 COC(=O)c1ccc(CNC2(c3nc(-c4ccc(C)cc4)c[nH]3)CCCC2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL412561 219783 0 None -7 3 Human 6.1 pKi = 6.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
44332643 11422 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 434 2 3 2 6.1 c1ccc(-c2c[nH]c(C3Cc4c([nH]c5ccccc45)C4(N3)C3CC5CC(C3)CC4C5)n2)cc1 10.1021/jm0108449
CHEMBL103088 11422 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 434 2 3 2 6.1 c1ccc(-c2c[nH]c(C3Cc4c([nH]c5ccccc45)C4(N3)C3CC5CC(C3)CC4C5)n2)cc1 10.1021/jm0108449
CHEMBL1202953 11422 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
ChEMBL 434 2 3 2 6.1 c1ccc(-c2c[nH]c(C3Cc4c([nH]c5ccccc45)C4(N3)C3CC5CC(C3)CC4C5)n2)cc1 10.1021/jm0108449
CHEMBL437220 220490 0 None -3 4 Human 7.1 pKi = 7.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
122186657 129677 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 349 6 2 4 4.2 CCn1cncc1CNC1(c2nc(-c3ccc(C)cc3)c[nH]2)CCCC1 10.1016/j.bmcl.2015.06.087
CHEMBL3605815 129677 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 349 6 2 4 4.2 CCn1cncc1CNC1(c2nc(-c3ccc(C)cc3)c[nH]2)CCCC1 10.1016/j.bmcl.2015.06.087
44377623 126694 0 None -16 2 Human 5.1 pKi = 5.1 Binding
Inhibitory constant on human somatostatin receptor type 3Inhibitory constant on human somatostatin receptor type 3
ChEMBL 449 9 2 6 4.7 CCCCNC(=O)C(C)(C)c1cn2cc(-c3csc4ccccc34)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
CHEMBL349355 126694 0 None -16 2 Human 5.1 pKi = 5.1 Binding
Inhibitory constant on human somatostatin receptor type 3Inhibitory constant on human somatostatin receptor type 3
ChEMBL 449 9 2 6 4.7 CCCCNC(=O)C(C)(C)c1cn2cc(-c3csc4ccccc34)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
90644976 118618 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 409 5 3 2 5.4 O=C(Nc1ccc(F)cc1)N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1 10.1021/ml500079u
CHEMBL3287647 118618 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 409 5 3 2 5.4 O=C(Nc1ccc(F)cc1)N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1 10.1021/ml500079u
122186638 129658 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 331 5 2 2 4.9 Cc1ccc(-c2c[nH]c(C3(NCc4ccccc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
CHEMBL3605796 129658 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 minsDisplacement of [125I]SS-14 from human SSTR3 expressed in CHO cells after 60 to 90 mins
ChEMBL 331 5 2 2 4.9 Cc1ccc(-c2c[nH]c(C3(NCc4ccccc4)CCCC3)n2)cc1 10.1016/j.bmcl.2015.06.087
90644986 118595 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 342 5 3 3 3.4 O=C(N[C@@H]1CCCC[C@@H]1NCc1cccc(O)c1)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287618 118595 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 342 5 3 3 3.4 O=C(N[C@@H]1CCCC[C@@H]1NCc1cccc(O)c1)c1ccc(F)cc1 10.1021/ml500079u
10009650 106571 0 None -8 4 Human 6.1 pKi = 6.1 Binding
Binding affinity for human receptor subtype hSSTR3.Binding affinity for human receptor subtype hSSTR3.
ChEMBL 668 20 3 8 6.1 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL285333 106571 0 None -8 4 Human 6.1 pKi = 6.1 Binding
Binding affinity for human receptor subtype hSSTR3.Binding affinity for human receptor subtype hSSTR3.
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
90645001 118613 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 352 5 2 2 3.8 O=C(N[C@@H]1C[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287637 118613 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 352 5 2 2 3.8 O=C(N[C@@H]1C[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL2369735 216442 0 None -16 5 Human 7.0 pKi = 7.0 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 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
CHEMBL510755 222367 0 None -3 3 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned sst3 receptorBinding affinity to human cloned sst3 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 216284 0 None -8 5 Human 7.0 pKi = 7.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
CHEMBL438726 220568 0 None -2 4 Human 7.0 pKi = 7.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 3The compound was tested for binding affinity against human Somatostatin receptor type 3
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
44397648 73538 0 None -24 5 Human 7.0 pKi = 7.0 Binding
Binding affinity against human sst3 receptor at 10 uMBinding affinity against human sst3 receptor at 10 uM
ChEMBL 476 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3c(Cl)cccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL185861 73538 0 None -24 5 Human 7.0 pKi = 7.0 Binding
Binding affinity against human sst3 receptor at 10 uMBinding affinity against human sst3 receptor at 10 uM
ChEMBL 476 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3c(Cl)cccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
90645011 118600 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 376 5 2 2 4.8 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccccc1 10.1021/ml500079u
CHEMBL3287625 118600 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 376 5 2 2 4.8 O=C(N[C@@H]1CCCC[C@@H]1NCc1ccc(Cl)c(Cl)c1)c1ccccc1 10.1021/ml500079u
16161315 222875 0 None -1 13 Mouse 8.0 pIC50 = 8 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3
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
2055 9682 48 None -66 14 Mouse 8.1 pIC50 = 8.1 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3
Drug Central None None None None None
383414 9682 48 None -66 14 Mouse 8.1 pIC50 = 8.1 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3
Drug Central None None None None None
90488715 9682 48 None -66 14 Mouse 8.1 pIC50 = 8.1 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3
Drug Central None None None None None
CHEMBL1680 9682 48 None -66 14 Mouse 8.1 pIC50 = 8.1 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3
Drug Central None None None None None
CHEMBL262746 9682 48 None -66 14 Mouse 8.1 pIC50 = 8.1 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3
Drug Central None None None None None
DB00104 9682 48 None -66 14 Mouse 8.1 pIC50 = 8.1 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3
Drug Central None None None None None
16161315 222875 0 125I-Tyr11-SRIF -1 13 Mouse 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 222875 0 125I-Tyr11-somatostatin -3 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
16161315 222875 0 125I-CGP23996 -1 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
16161315 222875 0 125I-Tyr11-SRIF-14 -4 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
16161315 222875 0 125I-Tyr11-somatostatin-14 -4 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
16161315 222875 0 125I-Tyr11-somatostatin-14 -3 13 Rat 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
16161315 222875 0 125I-CGP23996 -4 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 222875 0 125I-Tyr10-CST14 -4 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 222875 0 125I-Tyr10-CST14 -4 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 222875 0 125I-SOMATOSTATIN 14 -4 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 222875 0 125I-SRIF -4 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 222875 0 125I-SRIF-28 -4 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 222875 0 125I-LTT-SRIF28 -4 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 222875 0 125I-LTT-SRIF28 -4 13 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 UNDEFINED -4 13 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-Tyr11-SRIF -4 13 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-Tyr11-SRIF -4 13 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-LTT-SST-28 -4 13 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-LTT-SST-28 -4 13 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-Tyr11-SRIF -4 13 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-Tyr11-somatostatin-14 -1 13 Mouse 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-SOMATOSTATIN -3 13 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-Tyr11-somatostatin-14 -4 13 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 125I-LTT-SST-28 -4 13 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 222875 0 None -4 13 Human 8.0 pKi = 8 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) 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 7293 81 UNDEFINED -5754 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 7293 81 UNDEFINED -5754 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 7293 81 UNDEFINED -5754 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 7293 81 UNDEFINED -5754 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 7293 81 UNDEFINED -5754 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
46882665 12404 0 UNDEFINED -15 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 382 7 1 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cccnc4o3)CC2)ccc1OC None
CHEMBL1077721 12404 0 UNDEFINED -15 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 382 7 1 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cccnc4o3)CC2)ccc1OC None
46882666 12405 0 UNDEFINED -13 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 382 7 1 7 3.7 CCOc1cc(CN2CCC(Nc3nc4ccncc4o3)CC2)ccc1OC None
CHEMBL1077722 12405 0 UNDEFINED -13 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 382 7 1 7 3.7 CCOc1cc(CN2CCC(Nc3nc4ccncc4o3)CC2)ccc1OC None
46882746 12409 0 UNDEFINED -21 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 1 6 3.9 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OC None
CHEMBL1077742 12409 0 UNDEFINED -21 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 1 6 3.9 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OC None
24740861 12450 0 UNDEFINED -20 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 399 8 1 6 4.3 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCCF None
CHEMBL1077877 12450 0 UNDEFINED -20 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 399 8 1 6 4.3 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCCF None
46882789 12451 0 UNDEFINED -19 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 419 6 1 5 5.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1C(F)(F)F None
CHEMBL1077887 12451 0 UNDEFINED -19 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 419 6 1 5 5.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1C(F)(F)F None
46882181 12453 0 UNDEFINED -50 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 536 10 2 8 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5ccccc5)ccc4o3)CC2)ccc1OC None
CHEMBL1077908 12453 0 UNDEFINED -50 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 536 10 2 8 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5ccccc5)ccc4o3)CC2)ccc1OC None
46882790 12474 0 UNDEFINED -18 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 407 8 1 6 4.8 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC1CC1 None
CHEMBL1078081 12474 0 UNDEFINED -18 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 407 8 1 6 4.8 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC1CC1 None
46882620 12487 0 UNDEFINED -28 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 465 8 1 7 5.2 CCOc1cc(CN2CCC(Nc3nc4cc(OC(F)(F)F)ccc4o3)CC2)ccc1OC None
CHEMBL1078215 12487 0 UNDEFINED -28 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 465 8 1 7 5.2 CCOc1cc(CN2CCC(Nc3nc4cc(OC(F)(F)F)ccc4o3)CC2)ccc1OC None
46882664 12489 0 UNDEFINED -28 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 494 8 2 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1OC None
CHEMBL1078240 12489 0 UNDEFINED -28 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 494 8 2 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1OC None
46882621 12495 0 UNDEFINED -28 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 438 8 2 7 4.3 CCOc1cc(CN2CCC(Nc3nc4cc(NC(C)=O)ccc4o3)CC2)ccc1OC None
CHEMBL1078283 12495 0 UNDEFINED -28 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 438 8 2 7 4.3 CCOc1cc(CN2CCC(Nc3nc4cc(NC(C)=O)ccc4o3)CC2)ccc1OC None
46882831 12516 0 UNDEFINED -301 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 8 2 7 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OCC)c1N None
CHEMBL1078449 12516 0 UNDEFINED -301 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 8 2 7 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OCC)c1N None
46882832 12518 0 UNDEFINED -64 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 467 10 1 8 4.9 CCOC(=O)c1c(OCC)cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCC None
CHEMBL1078450 12518 0 UNDEFINED -64 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 467 10 1 8 4.9 CCOC(=O)c1c(OCC)cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCC None
11848626 12519 0 UNDEFINED -56 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 413 8 1 6 4.8 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OCC)c1F None
CHEMBL1078451 12519 0 UNDEFINED -56 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 413 8 1 6 4.8 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OCC)c1F None
46882622 12534 0 UNDEFINED -44 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 488 9 1 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)ccc1OC None
CHEMBL1078528 12534 0 UNDEFINED -44 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 488 9 1 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)ccc1OC None
11848625 12564 0 UNDEFINED -107 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 None
CHEMBL1078745 12564 0 UNDEFINED -107 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 None
46882708 12575 0 UNDEFINED -26 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 380 7 2 6 4.3 CCNc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
CHEMBL1078841 12575 0 UNDEFINED -26 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 380 7 2 6 4.3 CCNc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
11848833 12579 0 UNDEFINED -323 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 423 8 1 6 5.5 CC(C)Oc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC(C)C)c1 None
CHEMBL1078895 12579 0 UNDEFINED -323 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 423 8 1 6 5.5 CC(C)Oc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC(C)C)c1 None
46882133 12580 0 UNDEFINED -54 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 478 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NC(=O)C5CCC5)ccc4o3)CC2)ccc1OC None
CHEMBL1078896 12580 0 UNDEFINED -54 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 478 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NC(=O)C5CCC5)ccc4o3)CC2)ccc1OC None
46882445 12583 0 UNDEFINED -30 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 6 1 6 4.8 CCOc1cc(N2CCC(Nc3nc4ccccc4s3)CC2)ccc1OC None
CHEMBL1078903 12583 0 UNDEFINED -30 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 6 1 6 4.8 CCOc1cc(N2CCC(Nc3nc4ccccc4s3)CC2)ccc1OC None
46882180 12613 0 UNDEFINED -39 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 482 7 2 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1F None
CHEMBL1079180 12613 0 UNDEFINED -39 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 482 7 2 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1F None
46882577 12629 1 UNDEFINED -51 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 415 7 1 6 5.0 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)ccc4o3)CC2)ccc1OC None
CHEMBL1079312 12629 1 UNDEFINED -51 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 415 7 1 6 5.0 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)ccc4o3)CC2)ccc1OC None
46882578 12630 0 UNDEFINED -51 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 473 9 1 8 4.1 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)ccc1OC None
CHEMBL1079313 12630 0 UNDEFINED -51 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 473 9 1 8 4.1 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)ccc1OC None
46882579 12631 0 UNDEFINED -39 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 1 8 4.2 CCOc1cc(CN2CCC(Nc3nc4cc([N+](=O)[O-])ccc4o3)CC2)ccc1OC None
CHEMBL1079314 12631 0 UNDEFINED -39 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 1 8 4.2 CCOc1cc(CN2CCC(Nc3nc4cc([N+](=O)[O-])ccc4o3)CC2)ccc1OC None
46882182 12693 0 UNDEFINED -190 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 567 11 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)cc(OCC)c1-n1cccc1 None
CHEMBL1079686 12693 0 UNDEFINED -190 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 567 11 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)cc(OCC)c1-n1cccc1 None
16062555 12728 0 UNDEFINED -562 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 457 9 2 7 4.5 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)cc(OCC)c1F None
CHEMBL1079874 12728 0 UNDEFINED -562 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 457 9 2 7 4.5 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)cc(OCC)c1F None
11848835 12835 0 UNDEFINED -1258 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 456 9 2 7 3.9 CCOc1cc(CN2CCC(Nc3nc4cc(C(N)=O)ccc4o3)CC2)cc(OCC)c1F None
CHEMBL1080584 12835 0 UNDEFINED -1258 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 456 9 2 7 3.9 CCOc1cc(CN2CCC(Nc3nc4cc(C(N)=O)ccc4o3)CC2)cc(OCC)c1F None
16062816 12836 0 UNDEFINED -3311 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 473 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(C(=O)O)ccc4o3)CC2)cc(OCC)c1Cl None
CHEMBL1080585 12836 0 UNDEFINED -3311 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 473 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(C(=O)O)ccc4o3)CC2)cc(OCC)c1Cl None
16062553 12837 0 UNDEFINED -436 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 429 7 2 6 4.7 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)ccc1Cl None
CHEMBL1080586 12837 0 UNDEFINED -436 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 429 7 2 6 4.7 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)ccc1Cl None
46882225 12919 0 UNDEFINED -39 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 526 9 2 8 4.1 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)cc(OCC)c1F None
CHEMBL1080950 12919 0 UNDEFINED -39 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 526 9 2 8 4.1 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)cc(OCC)c1F None
46882226 12920 0 UNDEFINED -41 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 419 6 1 5 5.6 CCOc1cc(CN2CCC(Nc3nc4ccc(Cl)cc4o3)CC2)ccc1Cl None
CHEMBL1080951 12920 0 UNDEFINED -41 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 419 6 1 5 5.6 CCOc1cc(CN2CCC(Nc3nc4ccc(Cl)cc4o3)CC2)ccc1Cl None
46882227 12948 0 UNDEFINED -57 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 540 10 2 10 3.8 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5cn(C)cn5)ccc4o3)CC2)ccc1OC None
CHEMBL1081133 12948 0 UNDEFINED -57 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 540 10 2 10 3.8 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5cn(C)cn5)ccc4o3)CC2)ccc1OC None
46882517 12987 0 UNDEFINED -32 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 398 7 1 7 4.2 CCOc1cc(CN2CCC(Nc3nc4cccnc4s3)CC2)ccc1OC None
CHEMBL1081317 12987 0 UNDEFINED -32 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 398 7 1 7 4.2 CCOc1cc(CN2CCC(Nc3nc4cccnc4s3)CC2)ccc1OC None
46882224 13120 0 UNDEFINED -181 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 543 10 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)cc(OC2CCOCC2)c1 None
CHEMBL1082036 13120 0 UNDEFINED -181 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 543 10 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)cc(OC2CCOCC2)c1 None
46882516 13121 0 UNDEFINED -27 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 431 7 1 6 5.4 CCOc1cc(CN2CCC(Nc3nc4ccc(Cl)cc4s3)CC2)ccc1OC None
CHEMBL1082040 13121 0 UNDEFINED -27 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 431 7 1 6 5.4 CCOc1cc(CN2CCC(Nc3nc4ccc(Cl)cc4s3)CC2)ccc1OC None
11848624 95921 0 UNDEFINED -245 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
CHEMBL236587 95921 0 UNDEFINED -245 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
24740752 95922 0 UNDEFINED -436 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 409 8 1 6 4.9 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCC(C)C None
CHEMBL236588 95922 0 UNDEFINED -436 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 409 8 1 6 4.9 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCC(C)C None
24740863 95933 0 UNDEFINED -134 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl None
CHEMBL236610 95933 0 UNDEFINED -134 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl None
24740864 95934 0 UNDEFINED -269 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 365 6 1 5 4.6 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1C None
CHEMBL236611 95934 0 UNDEFINED -269 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 365 6 1 5 4.6 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1C None
11848679 96019 0 UNDEFINED -776 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 489 9 3 9 2.9 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)cc(OCC)c1N None
CHEMBL236788 96019 0 UNDEFINED -776 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 489 9 3 9 2.9 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)cc(OCC)c1N None
24740750 96482 0 UNDEFINED -151 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 6 4.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1O None
CHEMBL237660 96482 0 UNDEFINED -151 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 6 4.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1O None
24740753 152895 0 UNDEFINED -33 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 8 1 6 4.7 CCCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
CHEMBL391951 152895 0 UNDEFINED -33 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 8 1 6 4.7 CCCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
24740751 154659 0 UNDEFINED -120 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 421 7 1 6 5.2 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OC1CCCC1 None
CHEMBL393333 154659 0 UNDEFINED -120 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 421 7 1 6 5.2 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OC1CCCC1 None
24740862 154787 0 UNDEFINED -51 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 6 1 5 4.4 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1F None
CHEMBL393436 154787 0 UNDEFINED -51 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 6 1 5 4.4 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1F None
11848677 155131 0 UNDEFINED -32 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 460 8 2 8 3.0 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)ccc1OC None
CHEMBL393718 155131 0 UNDEFINED -32 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 460 8 2 8 3.0 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)ccc1OC None
None 224403 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 6 1 6 4.8 CCOC1=C(C=CC(=C1)NC2CCN(CC2)C3=NC4=CC=CC=C4S3)OC None
None 224404 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 397 7 1 6 4.8 CCOC1=C(C=CC(=C1)NC2CCN(CC2)CC3=NC4=CC=CC=C4S3)OC None
None 224405 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 425 7 1 6 4.6 CCOC1=C(C=CC(=C1)CN2CCC(CC2)C(=O)NC3=NC4=CC=CC=C4S3)OC None
None 224406 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 397 7 2 6 5.5 CCOC1=C(C=CC(=C1)NC2CCC(CC2)NC3=NC4=CC=CC=C4S3)OC None
None 224407 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 411 8 2 6 5.2 CCOC1=C(C=CC(=C1)NC2CCC(CC2)NCC3=NC4=CC=CC=C4S3)OC None
None 224408 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 5 1 6 4.1 CCOC1=C(C=CC(=C1)N2CCN(CC2)C(=O)NC3=NC4=CC=CC=C4S3)OC None
None 224409 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 405 8 2 6 6.1 CCOC1=C(C=CC(=C1)NCC2=CC(=CC=C2)NC3=NC4=CC=CC=C4S3)OC None
None 224410 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 382 7 1 7 3.7 CCOC1=C(C=CC(=C1)CN2CCC(CC2)NC3=NC4=C(O3)C=CC=N4)OC None
None 224411 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 380 7 2 5 4.0 CCOC1=C(C=CC(=C1)CN2CCC(CC2)NC3=NC4=CC=CC=C4N3)OC None
None 224412 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 382 7 1 7 3.7 CCOC1=C(N=CC(=C1)CN2CCC(CC2)NC3=NC4=CC=CC=C4O3)OC None
None 224413 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 409 8 1 6 5.1 CCOC1=C(C=CC(=C1)CN2CCC(CC2)NC3=NC4=CC=CC=C4O3)OC(C)C None
None 224414 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 413 8 1 6 4.8 CCOC1=CC(=C(C(=C1)CN2CCC(CC2)NC3=NC4=CC=CC=C4O3)F)OCC None
None 224415 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 429 9 2 7 3.8 CCOC1=C(C=C(C(=C1)CN2CCC(CC2)NC3=NC4=CC=CC=C4O3)F)OCCO None
2055 9682 48 125I-Tyr11-SRIF -40 14 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-Tyr11-SRIF -40 14 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-Tyr11-SRIF -40 14 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-Tyr11-SRIF -40 14 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-Tyr11-SRIF -40 14 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-Tyr11-SRIF -40 14 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
None 222876 0 125I-CGP23996 -338 12 Mouse 7.9 pKi = 7.9 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
None 222876 0 125I-Tyr11-SRIF -338 12 Mouse 7.9 pKi = 7.9 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
2054 10746 15 125I-Tyr10-CST14 -72 11 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 125I-Tyr10-CST14 -72 11 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 125I-Tyr10-CST14 -72 11 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 125I-Tyr10-CST14 -72 11 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 125I-Tyr10-CST14 -72 11 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
13105142 222877 0 125I-Tyr10-CST14 -301 5 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 808 11 8 8 2.0 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O None
None 223127 0 125I-LTT-SST-28 91 5 Human 6.9 pKi = 6.9 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 223128 0 125I-LTT-SST-28 -3467 5 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 485 11 4 4 3.1 COC(=O)C(CCCN=C(N)N)NC(=O)CCCC1=C(NC2=C(C=C(C=C12)F)F)C3=CC=CC=C3 None
None 223128 0 UNDEFINED -3467 5 Human 5.9 pKi = 5.9 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
2055 9682 48 125I-LTT-SRIF28 -40 14 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-LTT-SRIF28 -40 14 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-LTT-SRIF28 -40 14 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-LTT-SRIF28 -40 14 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-LTT-SRIF28 -40 14 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-LTT-SRIF28 -40 14 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
13105142 222877 0 125I-LTT-SRIF28 -301 5 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 808 11 8 8 2.0 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O None
13105142 222877 0 125I-LTT-SRIF28 -301 5 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 808 11 8 8 2.0 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O None
2055 9682 48 125I-SOMATOSTATIN -37 14 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-SOMATOSTATIN -37 14 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-SOMATOSTATIN -37 14 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-SOMATOSTATIN -37 14 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-SOMATOSTATIN -37 14 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-SOMATOSTATIN -37 14 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 10746 15 125I-CGP23996 -72 11 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 125I-CGP23996 -72 11 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 125I-CGP23996 -72 11 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 125I-CGP23996 -72 11 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 125I-CGP23996 -72 11 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 125I-Tyr11-SRIF -40 14 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 125I-Tyr11-somatostatin-14 -66 14 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-Tyr11-SRIF -40 14 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-Tyr11-somatostatin-14 -66 14 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-Tyr11-SRIF -40 14 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-Tyr11-somatostatin-14 -66 14 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-Tyr11-SRIF -40 14 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-Tyr11-somatostatin-14 -66 14 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-Tyr11-SRIF -40 14 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-Tyr11-somatostatin-14 -66 14 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-Tyr11-SRIF -40 14 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-Tyr11-somatostatin-14 -66 14 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
None 223127 0 Functional 91 5 Human 7.7 pKi = 7.7 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
2054 10746 15 125I-SRIF -72 11 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 10746 15 125I-SRIF-28 -72 11 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 125I-SRIF -72 11 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 125I-SRIF-28 -72 11 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 125I-SRIF -72 11 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 125I-SRIF-28 -72 11 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 125I-SRIF -72 11 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 125I-SRIF-28 -72 11 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 125I-SRIF -72 11 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 125I-SRIF-28 -72 11 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 222875 0 125I-LTT-SST-28 -4 13 Human 8.7 pKi = 8.7 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
2055 9682 48 125I-Tyr10-CST14 -40 14 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-Tyr10-CST14 -40 14 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-Tyr10-CST14 -40 14 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-Tyr10-CST14 -40 14 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-Tyr10-CST14 -40 14 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-Tyr10-CST14 -40 14 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase None None None None None
None 222876 0 125I-Tyr11-SRIF -380 12 Human 7.7 pKi = 7.7 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
13105142 222877 0 125I-CGP23996 -301 5 Human 7.7 pKi = 7.7 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
2054 10746 15 125I-Tyr11-SRIF -77 11 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 125I-Tyr11-SRIF -77 11 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 125I-Tyr11-SRIF -77 11 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 125I-Tyr11-SRIF -77 11 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 125I-Tyr11-SRIF -77 11 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase None None None None None
None 222876 0 125I-LTT-SST-28 -380 12 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 223127 0 125I-LTT-SST-28 91 5 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 584 17 5 8 2.8 CCCCC(C(=O)NC(CCCCN)C(=O)OC)NC(=O)NC(CC1=CC=CC=C1)C(=O)NC2=CC=C(C=C2)[N+](=O)[O-] None
None 223127 0 UNDEFINED 91 5 Human 7.6 pKi = 7.6 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 222876 0 125I-Tyr11-SRIF -380 12 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 222876 0 125I-Tyr11-somatostatin-14 -338 12 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 222876 0 125I-LTT-SST-28 -380 12 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
13105142 222877 0 UNDEFINED -301 5 Human 7.6 pKi = 7.6 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
2055 9682 48 125I-CGP23996 -66 14 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-CGP23996 -66 14 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-CGP23996 -66 14 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-CGP23996 -66 14 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-CGP23996 -66 14 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-CGP23996 -66 14 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 125I-Tyr11-SRIF -66 14 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-Tyr11-SRIF -66 14 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-Tyr11-SRIF -66 14 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-Tyr11-SRIF -66 14 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-Tyr11-SRIF -66 14 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-Tyr11-SRIF -66 14 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 125I-CGP23996 -40 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-CGP23996 -40 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-CGP23996 -40 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-CGP23996 -40 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-CGP23996 -40 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-CGP23996 -40 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 222875 0 125I-Tyr11-SRIF -3 13 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
2054 10746 15 125I-LTT-SST-28 -72 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 125I-LTT-SST-28 -72 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 125I-LTT-SST-28 -72 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 125I-LTT-SST-28 -72 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 125I-LTT-SST-28 -72 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
None 223274 0 125I-LTT-SST-28 -6165 5 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 10746 15 UNDEFINED -72 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 UNDEFINED -72 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 UNDEFINED -72 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 UNDEFINED -72 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 UNDEFINED -72 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
None 222876 0 125I-SRIF -380 12 Human 7.5 pKi = 7.5 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
None 222876 0 125I-SRIF-28 -380 12 Human 7.5 pKi = 7.5 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 9682 48 125I-Tyr11-somatostatin-14 -40 14 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-Tyr11-somatostatin-14 -40 14 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-Tyr11-somatostatin-14 -40 14 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-Tyr11-somatostatin-14 -40 14 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-Tyr11-somatostatin-14 -40 14 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-Tyr11-somatostatin-14 -40 14 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
None 223125 0 125I-SOMATOSTATIN -4 9 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 1077 14 12 13 0.6 CC(C1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=CC=C4)CC5=CC=CC=C5)N)C(=O)N)CC6=CC=CC=C6)O None
2055 9682 48 125I-LTT-SST-28 -40 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 UNDEFINED -40 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-LTT-SST-28 -40 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 UNDEFINED -40 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-LTT-SST-28 -40 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 UNDEFINED -40 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-LTT-SST-28 -40 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 UNDEFINED -40 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-LTT-SST-28 -40 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 UNDEFINED -40 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-LTT-SST-28 -40 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 UNDEFINED -40 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 10746 15 125I-LTT-SRIF28 -72 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 125I-LTT-SRIF28 -72 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 125I-LTT-SRIF28 -72 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 125I-LTT-SRIF28 -72 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 125I-LTT-SRIF28 -72 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 10746 15 125I-LTT-SRIF28 -72 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 125I-LTT-SRIF28 -72 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 125I-LTT-SRIF28 -72 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 125I-LTT-SRIF28 -72 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 125I-LTT-SRIF28 -72 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
2031 9053 0 UNDEFINED -56 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
71349 9053 0 UNDEFINED -56 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB06791 9053 0 UNDEFINED -56 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 125I-LTT-SST-28 -40 14 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-LTT-SST-28 -40 14 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-LTT-SST-28 -40 14 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-LTT-SST-28 -40 14 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-LTT-SST-28 -40 14 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-LTT-SST-28 -40 14 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
None 222876 0 125I-SOMATOSTATIN -269 12 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
2055 9682 48 125I-SOMATOSTATIN 14 -40 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 125I-SRIF -40 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 125I-SRIF-28 -40 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-SOMATOSTATIN 14 -40 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-SRIF -40 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-SRIF-28 -40 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-SOMATOSTATIN 14 -40 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-SRIF -40 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-SRIF-28 -40 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-SOMATOSTATIN 14 -40 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-SRIF -40 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-SRIF-28 -40 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-SOMATOSTATIN 14 -40 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-SRIF -40 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-SRIF-28 -40 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-SOMATOSTATIN 14 -40 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-SRIF -40 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-SRIF-28 -40 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 9682 48 125I-LTT-SST-28 -40 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 9682 48 125I-LTT-SST-28 -40 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 9682 48 125I-LTT-SST-28 -40 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 9682 48 125I-LTT-SST-28 -40 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 9682 48 125I-LTT-SST-28 -40 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 9682 48 125I-LTT-SST-28 -40 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase None None None None None
154734381 224493 0 None -1 9 Rat 8.2 pKi = 8.2 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 223125 0 125I-Tyr11-somatostatin-14 -67 9 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 1077 14 12 13 0.6 CC(C1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=CC=C4)CC5=CC=CC=C5)N)C(=O)N)CC6=CC=CC=C6)O None
None 223125 0 UNDEFINED -67 9 Human 7.2 pKi = 7.2 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 223129 0 125I-LTT-SST-28 -89 5 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 536 11 4 5 5.2 CC(COC(=O)C(CCCCN)NC(=O)CC1=C(NC2=C1C=CC3=CC=CC=C32)C4=CC5=CC=CC=C5C=C4)N None
None 223129 0 UNDEFINED -89 5 Human 7.2 pKi = 7.2 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
2055 9682 48 None -37 14 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
383414 9682 48 None -37 14 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
90488715 9682 48 None -37 14 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
CHEMBL1680 9682 48 None -37 14 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
CHEMBL262746 9682 48 None -37 14 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
DB00104 9682 48 None -37 14 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
None 223126 0 125I-LTT-SST-28 -14454 5 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 585 8 5 5 4.2 CC(C1=CNC2=CC=CC=C21)C(C(=O)NCC3CCCC(C3)CN)NC(=O)N4CCC(CC4)N5C6=CC=CC=C6NC5=O None
None 223126 0 UNDEFINED -14454 5 Human 6.1 pKi = 6.1 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
154734381 224493 0 None -1 9 Human 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
2055 9682 48 None -40 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
383414 9682 48 None -40 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
90488715 9682 48 None -40 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
CHEMBL1680 9682 48 None -40 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
CHEMBL262746 9682 48 None -40 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
DB00104 9682 48 None -40 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
2054 10746 15 125I-SOMATOSTATIN -281 11 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 10746 15 125I-SOMATOSTATIN -281 11 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 10746 15 125I-SOMATOSTATIN -281 11 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 10746 15 125I-SOMATOSTATIN -281 11 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 10746 15 125I-SOMATOSTATIN -281 11 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase None None None None None
2052 9521 0 None -3 2 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2028 8288 0 None -112 6 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
2029 9154 0 None -56 6 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
2047 8996 0 None -56 4 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2047 8996 0 None -56 4 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2031 9053 0 None -213 9 Rat 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
71349 9053 0 None -213 9 Rat 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
DB06791 9053 0 None -213 9 Rat 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2032 7424 0 None -251 7 Rat 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2066 9940 0 None -7 4 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9544214
2067 9941 0 None -3 3 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9544214
2036 7430 0 None -4 5 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2036 7430 0 None -4 5 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2054 10746 15 None -281 11 Rat 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
71306 10746 15 None -281 11 Rat 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL264186 10746 15 None -281 11 Rat 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL3349523 10746 15 None -281 11 Rat 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
DB04894 10746 15 None -281 11 Rat 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2051 10349 24 None -218 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2051 10349 24 None -218 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2051 10349 24 None -218 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2051 10349 24 None -218 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2051 10349 24 None -218 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
5311430 10349 24 None -218 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
5311430 10349 24 None -218 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
5311430 10349 24 None -218 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
5311430 10349 24 None -218 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
5311430 10349 24 None -218 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
CHEMBL311695 10349 24 None -218 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL311695 10349 24 None -218 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL311695 10349 24 None -218 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL311695 10349 24 None -218 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL311695 10349 24 None -218 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
2051 10349 24 None -208 9 Rat 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
5311430 10349 24 None -208 9 Rat 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL311695 10349 24 None -208 9 Rat 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2034 7426 0 None -1 4 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2034 7426 0 None -1 4 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2073 9036 0 None - 1 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 584 17 5 8 2.8 NCCCC[C@@H](C(=O)OC)NC(=O)[C@H](NC(=O)N[C@H](C(=O)Nc1ccc(cc1)[N+](=O)[O-])Cc1ccccc1)CCCC 9784130
5311373 9036 0 None - 1 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 584 17 5 8 2.8 NCCCC[C@@H](C(=O)OC)NC(=O)[C@H](NC(=O)N[C@H](C(=O)Nc1ccc(cc1)[N+](=O)[O-])Cc1ccccc1)CCCC 9784130
2054 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2054 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2054 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
71306 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
71306 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
71306 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL264186 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL264186 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL264186 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL3349523 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL3349523 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL3349523 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
DB04894 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
DB04894 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
DB04894 10746 15 None -72 11 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2003 7428 0 None -10 2 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2055 9682 48 None -37 14 Rat 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
383414 9682 48 None -37 14 Rat 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
90488715 9682 48 None -37 14 Rat 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL1680 9682 48 None -37 14 Rat 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL262746 9682 48 None -37 14 Rat 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
DB00104 9682 48 None -37 14 Rat 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
11443899 7054 0 None - 1 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 526 7 0 5 4.6 COc1ccc(cn1)CC(CN1C[C@@H]2CCCC[C@@H]2[C@@H](C1)C(=O)N1CCN(CC1)c1ccc(c(c1)F)F)C None
2076 7054 0 None - 1 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 526 7 0 5 4.6 COc1ccc(cn1)CC(CN1C[C@@H]2CCCC[C@@H]2[C@@H](C1)C(=O)N1CCN(CC1)c1ccc(c(c1)F)F)C None
2014 8995 0 None -4 9 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2014 8995 0 None -4 9 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2017 9520 0 None -2 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2032 7424 0 None -19 7 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2035 7427 0 None -3 2 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2069 7439 0 None -1 2 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2040 7435 0 None -2 4 Rat 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2004 7429 0 None -3 7 Rat 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2068 7431 0 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2040 7435 0 None -1 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2071 7485 0 None - 1 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 454 10 3 2 7.8 CCCCCC1(CCCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 11520208
5311378 7485 0 None - 1 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 454 10 3 2 7.8 CCCCCC1(CCCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 11520208
2004 7429 0 None 2 7 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2004 7429 0 None 2 7 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2004 7429 0 None 2 7 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
16130961 7678 0 None 1 6 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
16130961 7678 0 None 1 6 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2005 7678 0 None 1 6 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2005 7678 0 None 1 6 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2007 7953 0 None 2 6 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2007 7953 0 None 2 6 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2031 9053 0 None -56 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2031 9053 0 None -56 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2031 9053 0 None -56 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2031 9053 0 None -56 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
71349 9053 0 None -56 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
71349 9053 0 None -56 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
71349 9053 0 None -56 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
71349 9053 0 None -56 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
DB06791 9053 0 None -56 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
DB06791 9053 0 None -56 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
DB06791 9053 0 None -56 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
DB06791 9053 0 None -56 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2055 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2055 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2055 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8097479
2055 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2055 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2055 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
383414 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
383414 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
383414 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8097479
383414 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
383414 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
383414 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
90488715 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
90488715 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
90488715 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8097479
90488715 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
90488715 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
90488715 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
CHEMBL1680 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL1680 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL1680 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8097479
CHEMBL1680 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL1680 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL1680 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
CHEMBL262746 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL262746 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL262746 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8097479
CHEMBL262746 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL262746 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL262746 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
DB00104 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
DB00104 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
DB00104 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8097479
DB00104 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
DB00104 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
DB00104 9682 48 None -40 14 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
2019 10447 0 None -10 10 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
44386062 10447 0 None -10 10 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL440072 10447 0 None -10 10 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
16133849 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
16133849 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
16133849 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
16133849 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8097479
16133849 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
16133849 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
16133849 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2020 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2020 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
2020 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2020 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8097479
2020 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2020 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2020 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
91935900 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
91935900 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
91935900 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
91935900 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8097479
91935900 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
91935900 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
91935900 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL501796 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL501796 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
CHEMBL501796 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL501796 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8097479
CHEMBL501796 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL501796 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL501796 10448 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
16133849 10448 12 None -5 9 Rat 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2020 10448 12 None -5 9 Rat 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
91935900 10448 12 None -5 9 Rat 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL501796 10448 12 None -5 9 Rat 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2070 7484 5 None 3467 4 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 11520208
9802572 7484 5 None 3467 4 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 11520208
CHEMBL2069499 7484 5 None 3467 4 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 11520208
2008 7994 0 None -1 6 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2008 7994 0 None -1 6 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
2008 7994 0 None -1 6 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2019 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2019 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11520208
2019 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
2019 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2019 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8097479
2019 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2019 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2019 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
2019 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
44386062 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
44386062 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11520208
44386062 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
44386062 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
44386062 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8097479
44386062 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
44386062 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
44386062 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
44386062 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
CHEMBL440072 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL440072 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11520208
CHEMBL440072 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
CHEMBL440072 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL440072 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8097479
CHEMBL440072 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL440072 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL440072 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
CHEMBL440072 10447 0 None 1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130