Ligand source activities (1 row/activity)



Get vendors


Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
42637503 195817 0 None 100 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14
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 195817 0 None 100 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14
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
CHEMBL563125 215746 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14
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](c2c[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
42637069 195509 0 None 48 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14
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 195509 0 None 48 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14
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
CHEMBL556949 215736 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14
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/jm801314f
68254010 166414 0 None -1778 3 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human SSTR1 expressed in CHO-K1 cell membranesAntagonist activity at human SSTR1 expressed in CHO-K1 cell membranes
ChEMBL 559 10 2 7 6.6 CCOc1cc(CN2CC[C@H]3C(Nc4nc5ccc(C(=O)O)cc5o4)CC[C@H]32)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4277106 166414 0 None -1778 3 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human SSTR1 expressed in CHO-K1 cell membranesAntagonist activity at human SSTR1 expressed in CHO-K1 cell membranes
ChEMBL 559 10 2 7 6.6 CCOc1cc(CN2CC[C@H]3C(Nc4nc5ccc(C(=O)O)cc5o4)CC[C@H]32)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
145705877 217736 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
2027 655 0 None -398 5 Human 5.6 pIC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11897676
2003 641 0 None -79 2 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8100350
2006 906 0 None -15 2 Rat 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9166718
2010 1376 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15658864
2011 1374 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15658865
2018 3007 28 None -63 5 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15477717
9941444 3007 28 None -63 5 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15477717
CHEMBL3349607 3007 28 None -63 5 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15477717
DB06663 3007 28 None -63 5 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15477717
2025 1281 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15658865
2009 1373 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15658865
2013 2180 0 None -3 6 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12450568
2012 1375 0 None 1 4 Human 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15658864
2026 654 0 None -31 5 Human 6.0 pIC50 None 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11897676
2019 3675 0 None -50 4 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9166718
44386062 3675 0 None -50 4 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9166718
CHEMBL440072 3675 0 None -50 4 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9166718
2006 906 0 None 15 2 Human 8.5 pIC50 None 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011


Get vendors


Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Similar-
ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay
Type		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
124168080 181834 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human SST1Agonist activity at human SST1
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 181834 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human SST1Agonist activity at human SST1
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 209031 40 None -6 5 Human 9.9 pIC50 = 9.9 Binding
Binding affinity to Somatostatin receptor type 1 (unknown origin) by radioligand displacement assayBinding affinity to Somatostatin receptor type 1 (unknown origin) by radioligand displacement assay
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmc.2013.03.016
CHEMBL1823872 209031 40 None -6 5 Human 9.9 pIC50 = 9.9 Binding
Binding affinity to Somatostatin receptor type 1 (unknown origin) by radioligand displacement assayBinding affinity to Somatostatin receptor type 1 (unknown origin) by radioligand displacement assay
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmc.2013.03.016
42637503 195817 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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 195817 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
45268875 195610 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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 195610 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
CHEMBL408338 212706 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
45268875 195610 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity to sst1 receptor in human prostate cancer cells by autoradiographyBinding affinity to sst1 receptor in human prostate cancer cells 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 195610 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity to sst1 receptor in human prostate cancer cells by autoradiographyBinding affinity to sst1 receptor in human prostate cancer cells 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
42637069 195509 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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 195509 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
CHEMBL409100 212746 0 None - 0 Human 9.0 pIC50 = 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 1.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 1.
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+
70689723 73968 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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 73968 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
16129706 209031 40 None -6 5 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO 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 209031 40 None -6 5 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO 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
16129706 209031 40 None -6 5 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[LTT]-SS28 from human SST1 receptor expressed in CHO cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST1 receptor expressed in CHO 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 209031 40 None -6 5 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[LTT]-SS28 from human SST1 receptor expressed in CHO cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST1 receptor expressed in CHO 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 213913 0 None -6 5 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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
16129706 209031 40 None -6 5 Human 8.7 pIC50 = 8.7 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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 209031 40 None -6 5 Human 8.7 pIC50 = 8.7 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL262379 210538 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL425465 213335 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL3350911 211529 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
118718507 115358 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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 115358 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (hsst) receptor
ChEMBL 1050 14 11 12 3.4 CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)NC(C)(C)C)NC1=O 10.1021/jm970730q
CHEMBL2079558 209194 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL3349505 211410 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL3349506 211411 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL3349508 211413 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (hsst) receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/jm970730q
CHEMBL3349597 211426 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (hsst) receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/jm970730q
CHEMBL3349608 211436 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (hsst) receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2cccnc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm970730q
CHEMBL3349610 211437 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(C)(C)SSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm970730q
CHEMBL3349611 211438 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (hsst) receptor
ChEMBL None None None CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm970730q
CHEMBL3349612 211439 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccccc2)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm970730q
CHEMBL3349613 211440 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL3349617 211443 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (hsst) receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2cccnc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm970730q
CHEMBL3349618 211444 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (hsst) receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2cccnc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm970730q
CHEMBL3349663 211447 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2cccc(-c3ccccc3)c2)CSSC[C@@H](C(=O)N[C@@H](Cc2cccc(-c3ccccc3)c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL3349665 211449 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL3349668 211452 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL3349673 211456 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL3349674 211457 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (hsst) receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/jm970730q
CHEMBL3349675 211458 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL3349678 211461 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL3349680 211463 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
49865345 15911 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST1 receptor expressed in CHO cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST1 receptor expressed in CHO 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 15911 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST1 receptor expressed in CHO cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST1 receptor expressed in CHO 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
CHEMBL3349667 211451 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL412629 213012 0 None - 0 Human 7.0 pIC50 = 7 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 1.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 1.
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+
CHEMBL3349679 211462 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL408825 212734 0 None - 0 Human 7.0 pIC50 = 7.0 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 1.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 1.
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm010037+
CHEMBL2374244 210383 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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]3CCC(=O)NCC[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)N3)cc1 10.1021/jm049519m
CHEMBL3349507 211412 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (hsst) receptor
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
162646037 179514 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR1 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR1 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 179514 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR1 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR1 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
25188780 12431 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12431 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12431 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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
CHEMBL540408 215714 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiography
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL3349666 211450 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL410047 212797 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL408611 212723 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CN[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](Cc2ccc(CNC(C)C)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm049520l
CHEMBL3350881 211504 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
CHEMBL3350895 211517 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
CHEMBL426698 213348 0 None - 0 Human 6.9 pIC50 = 6.9 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 1.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 1.
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+
122179477 121474 5 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of SSTR1 receptor (unknown origin)Inhibition of SSTR1 receptor (unknown origin)
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 121474 5 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of SSTR1 receptor (unknown origin)Inhibition of SSTR1 receptor (unknown origin)
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
CHEMBL1824049 209033 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO 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
CHEMBL3122130 211108 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[LTT]-SS28 from human SST1 receptor expressed in CHO cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST1 receptor expressed in CHO 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
CHEMBL500326 214111 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptorDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 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(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL554624 215726 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
CHEMBL556949 215736 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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](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/jm801314f
CHEMBL387005 212403 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL411002 212856 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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/jm049519m
CHEMBL265120 210637 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CN[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](Cc2ccc(CNC(C)C)cc2)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
CHEMBL411002 212856 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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/jm049520l
CHEMBL1824050 209034 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO 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
CHEMBL3349671 211454 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL410144 212801 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL385811 212368 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL436887 213691 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL414749 213153 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 1.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 1.
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+
CHEMBL438776 213798 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 1.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 1.
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+
CHEMBL555737 215731 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
CHEMBL414716 213149 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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)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
CHEMBL2079563 209196 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL446380 213945 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptorDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptor
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
44388108 161695 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL413413 161695 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL414692 213147 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)O)CSSC[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049520l
CHEMBL3351090 211544 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
44388133 167203 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1710 22 21 22 -0.9 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCCC(=O)NCCC[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
CHEMBL429164 167203 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1710 22 21 22 -0.9 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCCC(=O)NCCC[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
CHEMBL563461 215748 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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](Cc3ccc(O)cc3)NC(=O)[C@](C)([C@@H](C)O)NC2=O)cc1 10.1021/jm801314f
CHEMBL268205 210743 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL436887 213691 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 1.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 1.
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm010037+
CHEMBL440083 213861 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 1.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 1.
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](CCCCNC(N)=O)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/jm010037+
CHEMBL3122129 211107 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[LTT]-SS28 from human SST1 receptor expressed in CHO cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST1 receptor expressed in CHO 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
CHEMBL437905 213738 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)N(C)C(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL3122124 211103 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[LTT]-SS28 from human SST1 receptor expressed in CHO cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST1 receptor expressed in CHO 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
CHEMBL409952 212787 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]([C@@H](C)O)NC2=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](Cc2ccccc2)C(=O)N3)cc1 10.1021/jm049519m
CHEMBL2373256 210373 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCCC[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(N)=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
25188220 12491 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12491 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12491 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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
CHEMBL407858 212690 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 1.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 1.
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+
42637283 195514 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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 195514 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
CHEMBL559150 215744 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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 210666 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL386784 212392 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL442494 213913 0 None -6 5 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human sst1 by in vitro receptor autoradiography assayBinding affinity to human sst1 by in vitro receptor autoradiography assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/ml200032v
CHEMBL442494 213913 0 None -6 5 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst1 receptor expressed in CHOK1 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst1 receptor expressed in CHOK1 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
CHEMBL1823873 209032 9 None 1 4 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO 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
CHEMBL442494 213913 0 None -6 5 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst1 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst1 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 213913 0 None -6 5 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST1 receptor expressed in CHO cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST1 receptor expressed in CHO 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
CHEMBL1909004 209074 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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 209074 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
CHEMBL413419 213065 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL263340 210568 0 None - 0 Human 8.6 pIC50 = 8.6 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 1.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 1.
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+
CHEMBL1824051 209035 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO 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 213913 0 None -6 5 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst1 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst1 receptor by autoradiography
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm701618q
CHEMBL442494 213913 0 None -6 5 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
45273131 194786 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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 194786 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
CHEMBL2311181 209507 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
156009460 178225 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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 178225 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL439135 213826 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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]3CCC(=O)NCCCC[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)N3)cc1 10.1021/jm049519m
CHEMBL3350897 211519 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
CHEMBL3350899 211521 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
CHEMBL3349614 211441 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL504248 214175 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptorDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptor
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
CHEMBL504457 214177 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptorDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptor
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
CHEMBL440066 213858 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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](Cc3ccc4ccccc4c3)C(=O)N2C)cc1 10.1021/jm049520l
CHEMBL413442 213072 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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)N(C)C(=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
122179457 121454 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to somatostatin receptor type 1 (unknown origin)Binding affinity to somatostatin receptor type 1 (unknown origin)
ChEMBL 495 4 3 8 3.7 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL3582317 121454 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to somatostatin receptor type 1 (unknown origin)Binding affinity to somatostatin receptor type 1 (unknown origin)
ChEMBL 495 4 3 8 3.7 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
16737814 85507 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 85507 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 85507 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 85507 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST1 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST1 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 85507 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST1 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST1 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 85507 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST1 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST1 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
10114 2556 23 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]SS-28 from human SSTR-1 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR-1 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 2556 23 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]SS-28 from human SSTR-1 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR-1 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 2556 23 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]SS-28 from human SSTR-1 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR-1 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
CHEMBL405784 212579 0 None - 0 Human 7.6 pIC50 = 7.6 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 1.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 1.
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+
CHEMBL407027 212633 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCC[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
CHEMBL3349669 211453 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL265615 210657 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 1.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 1.
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+
25187683 12451 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cells
ChEMBL 627 12 4 4 5.2 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1186082 12451 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cells
ChEMBL 627 12 4 4 5.2 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL448713 12451 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cells
ChEMBL 627 12 4 4 5.2 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL410428 212820 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
49865343 15909 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST1 receptor expressed in CHO cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST1 receptor expressed in CHO 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 15909 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST1 receptor expressed in CHO cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST1 receptor expressed in CHO 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
CHEMBL384195 212319 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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(=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](Cc3ccc4ccccc4c3)C(=O)N2C)cc1 10.1021/jm049520l
25187396 12684 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cells
ChEMBL 475 9 4 4 2.4 CC(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)NCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1187397 12684 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cells
ChEMBL 475 9 4 4 2.4 CC(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)NCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL501699 12684 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cells
ChEMBL 475 9 4 4 2.4 CC(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)NCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL5282589 194164 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human somatostatin receptor type 1Inhibition of human somatostatin receptor type 1
ChEMBL 633 14 7 7 0.1 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C1=O 10.1021/acs.jmedchem.6b01029
CHEMBL262551 210541 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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)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
44388036 160252 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1645 18 19 20 -0.3 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](Cc4ccc(O)cc4I)NC(=O)[C@@H]([C@@H](C)O)NC2=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](Cc2ccccc2)C(=O)N3)cc1 10.1021/jm049519m
CHEMBL411001 160252 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1645 18 19 20 -0.3 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](Cc4ccc(O)cc4I)NC(=O)[C@@H]([C@@H](C)O)NC2=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](Cc2ccccc2)C(=O)N3)cc1 10.1021/jm049519m
CHEMBL438576 213779 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)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
59568713 132128 15 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of somatostatin receptor subtype 1 (unknown origin)Inhibition of somatostatin receptor subtype 1 (unknown origin)
ChEMBL 466 6 2 8 2.0 Cc1c([C@@H](O)CN2CCN(C[C@H](O)c3ccc4c(c3C)COC4=O)CC2)ccc2c1COC2=O 10.1021/acsmedchemlett.6b00122
CHEMBL3696475 132128 15 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of somatostatin receptor subtype 1 (unknown origin)Inhibition of somatostatin receptor subtype 1 (unknown origin)
ChEMBL 466 6 2 8 2.0 Cc1c([C@@H](O)CN2CCN(C[C@H](O)c3ccc4c(c3C)COC4=O)CC2)ccc2c1COC2=O 10.1021/acsmedchemlett.6b00122
70683416 73967 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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 73967 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
CHEMBL425090 213329 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human Somatostatin receptor type 1 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 1 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL452157 213976 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human Somatostatin receptor type 1 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 1 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
CHEMBL3350898 211520 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
CHEMBL452157 213976 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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 213976 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO 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
25187400 12694 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12694 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12694 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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
CHEMBL452157 213976 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptorDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 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(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL452157 213976 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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 213976 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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 210671 0 None - 0 Human 7.6 pIC50 = 7.6 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 1.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 1.
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+
CHEMBL3350894 211516 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
44388134 141415 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1710 22 21 22 -0.9 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCC(=O)NCCCC[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
CHEMBL384072 141415 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1710 22 21 22 -0.9 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCC(=O)NCCCC[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
46902023 17038 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]iodotyrosyl from human SST1 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST1 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 17038 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]iodotyrosyl from human SST1 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST1 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
CHEMBL1907758 209068 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
CHEMBL442494 213913 0 None -6 5 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptorDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 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/jm701444y
CHEMBL442494 213913 0 None -6 5 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
16151826 195856 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiography
ChEMBL 1555 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm801314f
CHEMBL558600 195856 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiography
ChEMBL 1555 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm801314f
44388121 166722 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 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1555 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL428295 166722 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 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL1908981 209070 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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](Cc3ccc(O)c(I)c3)NC(=O)[C@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm801314f
CHEMBL539710 209070 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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](Cc3ccc(O)c(I)c3)NC(=O)[C@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm801314f
CHEMBL1907758 209068 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 1 expressed in CHO-K1 cells; (n=5)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 1 expressed in CHO-K1 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
CHEMBL386922 212401 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 1.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 1.
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm010037+
CHEMBL1907758 209068 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity at human Somatostatin receptor type 1 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 1 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
CHEMBL1907758 209068 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human Somatostatin receptor type 1 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 1 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
CHEMBL409653 212775 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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)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
CHEMBL414571 213144 0 None - 0 Human 7.5 pIC50 = 7.5 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 1.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 1.
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+
CHEMBL447989 213953 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptorDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptor
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
CHEMBL265846 210667 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 1.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 1.
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+
CHEMBL552013 215721 3 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
CHEMBL3349664 211448 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL2371059 210006 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
CHEMBL407125 212643 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 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3ccc4ccccc4c3)N(C)C(=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
CHEMBL3350905 211524 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
CHEMBL3122123 211102 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-[LTT]-SS28 from human SST1 receptor expressed in CHO cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST1 receptor expressed in CHO 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
CHEMBL386023 212373 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL413441 213071 0 None - 0 Human 7.5 pIC50 = 7.5 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 1.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 1.
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+
CHEMBL3350884 211507 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
CHEMBL428799 213471 0 None - 0 Human 7.5 pIC50 = 7.5 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 1.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 1.
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+
CHEMBL3350891 211514 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
CHEMBL437451 213720 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 1.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 1.
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+
CHEMBL404819 212534 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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)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
CHEMBL413378 213063 0 None - 0 Human 7.5 pIC50 = 7.5 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 1.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 1.
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+
CHEMBL1908984 209072 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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 209072 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
CHEMBL504395 214176 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptorDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptor
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
42637136 196504 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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 196504 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
25189054 12704 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12704 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12704 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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
25187955 12436 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12436 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12436 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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
CHEMBL3122127 211105 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[LTT]-SS28 from human SST1 receptor expressed in CHO cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST1 receptor expressed in CHO 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
25187679 12671 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12671 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12671 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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
25189327 12696 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12696 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12696 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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
118719101 115440 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1356 21 16 16 2.5 CNc1ccc(C(C(C)C)[C@@H]2NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC2=O)cc1 10.1021/jm030245x
CHEMBL3350724 115440 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1356 21 16 16 2.5 CNc1ccc(C(C(C)C)[C@@H]2NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC2=O)cc1 10.1021/jm030245x
CHEMBL1824052 209036 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO 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
42637563 195510 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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 195510 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
44388124 159370 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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 159370 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
44325273 207308 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration required for somatostatin 1 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 1 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 207308 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration required for somatostatin 1 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 1 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
CHEMBL2111257 209216 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity at human Somatostatin receptor type 1 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 1 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@H](C)c2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0302445
CHEMBL3350357 211475 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Somatostatin receptor type 1 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 1 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 215631 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptorDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptor
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
CHEMBL415144 213172 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(N)=O)CSSC[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3I)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049520l
CHEMBL2369510 209631 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 1.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 1.
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](CC(N)=O)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+
CHEMBL1909006 209075 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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 209075 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
44368406 10267 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Somatostatin receptor type 1 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 1 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1022 9 11 12 1.1 C[C@@H]1NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1161332 10267 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Somatostatin receptor type 1 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 1 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1022 9 11 12 1.1 C[C@@H]1NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL262790 210551 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(N)=O)CSSC[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049520l
CHEMBL3350886 211509 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
CHEMBL269485 210791 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 1.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 1.
ChEMBL None None None CCN(CC)C(=N)NCCCC[C@@H]1NC(=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)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC1=O 10.1021/jm010037+
CHEMBL2079559 209195 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
44388029 96454 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1659 18 18 20 0.0 CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3I)C(=O)N[C@H]3CCCCCCNC(=O)CC[C@@H](NC(=O)[C@@H](Cc4ccccc4)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC3=O)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049519m
CHEMBL262258 96454 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1659 18 18 20 0.0 CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3I)C(=O)N[C@H]3CCCCCCNC(=O)CC[C@@H](NC(=O)[C@@H](Cc4ccccc4)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC3=O)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049519m
CHEMBL2079626 209197 2 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL3350885 211508 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
CHEMBL2079558 209194 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL2079559 209195 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL407051 212634 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3I)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=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
CHEMBL406816 212623 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 1 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 1 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 209039 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 1 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 1 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 209039 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL1824055 209039 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO 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
CHEMBL216992 209348 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL2369533 209632 0 None - 0 Human 8.3 pIC50 = 8.3 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 1.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 1.
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+
CHEMBL406197 212598 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
10577746 207252 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration required for somatostatin 1 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 1 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 207252 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration required for somatostatin 1 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 1 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
CHEMBL3349677 211460 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
11563877 164720 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR1 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR1 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 164720 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR1 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR1 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
CHEMBL3350893 211515 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
CHEMBL413888 213096 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCCC[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
CHEMBL412473 212994 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)O)NC(=O)[C@H](CO)N(C)C(=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
42637210 195607 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
CHEMBL555956 195607 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
CHEMBL407120 212640 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 1.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 1.
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccc(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+
CHEMBL3349676 211459 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL406559 212613 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 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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)N(C)C(=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
25187398 12448 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12448 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12448 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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
CHEMBL503036 214160 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptorDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptor
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
CHEMBL415582 213190 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity at human Somatostatin receptor type 1 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 1 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL2371100 210012 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human Somatostatin receptor type 1 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 1 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
11468916 115463 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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 115463 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
CHEMBL441202 213884 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCC[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
71461685 79547 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 1.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 1.
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+
CHEMBL2114095 79547 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 1.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 1.
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+
49865347 15913 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST1 receptor expressed in CHO cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST1 receptor expressed in CHO 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 15913 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST1 receptor expressed in CHO cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST1 receptor expressed in CHO 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
122179477 121474 5 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]SS-14 from human recombinant SSTR1 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR1 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 121474 5 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]SS-14 from human recombinant SSTR1 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR1 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
CHEMBL415143 213171 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 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)N(C)C(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL3349672 211455 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
CHEMBL263587 210578 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL1908982 209071 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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 209071 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
CHEMBL411411 212884 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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]3CCC(=O)NCC[C@@H](NC(=O)[C@@H]([C@@H](C)O)NC2=O)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)O)CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@H](CCCCN)C(=O)N3)cc1 10.1021/jm049519m
CHEMBL1909003 209073 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiography
ChEMBL None None None CCCCCCC[C@@H]1NC(=O)[C@H](Cc2ccc(O)c(I)c2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(CNC(C)C)cc2)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC1=O 10.1021/jm801314f
CHEMBL540721 209073 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiography
ChEMBL None None None CCCCCCC[C@@H]1NC(=O)[C@H](Cc2ccc(O)c(I)c2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(CNC(C)C)cc2)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC1=O 10.1021/jm801314f
44388028 168767 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1645 18 19 20 -0.3 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](Cc4ccc(O)cc4I)NC(=O)[C@@H]([C@@H](C)O)NC2=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](Cc2ccccc2)C(=O)N3)cc1 10.1021/jm049519m
CHEMBL437348 168767 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1645 18 19 20 -0.3 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](Cc4ccc(O)cc4I)NC(=O)[C@@H]([C@@H](C)O)NC2=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](Cc2ccccc2)C(=O)N3)cc1 10.1021/jm049519m
CHEMBL3350912 211530 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
44388123 169186 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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 169186 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL2371051 210004 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity at human Somatostatin receptor type 1 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 1 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 209040 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO 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
44388120 178224 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1696 22 21 22 -1.3 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCCC(=O)NCC[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
CHEMBL4649895 178224 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1696 22 21 22 -1.3 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCCC(=O)NCC[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
CHEMBL414100 213109 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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]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
44388037 160979 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1659 18 18 20 0.0 CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3I)C(=O)N[C@@H]3CCCCCCNC(=O)CC[C@@H](NC(=O)[C@@H](Cc4ccccc4)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC3=O)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049519m
CHEMBL411600 160979 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1659 18 18 20 0.0 CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3I)C(=O)N[C@@H]3CCCCCCNC(=O)CC[C@@H](NC(=O)[C@@H](Cc4ccccc4)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC3=O)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049519m
25188218 12564 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12564 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12564 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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
44388132 97289 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1696 22 21 22 -1.3 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCC(=O)NCCC[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
CHEMBL269023 97289 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1696 22 21 22 -1.3 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCC(=O)NCCC[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 115460 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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 115460 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
44368019 10265 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Somatostatin receptor type 1 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 1 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1136 12 12 15 1.1 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)N(C(=O)c2ccccc2)C(=O)N(C)[C@H](O)NC(=O)[C@@H](N)CSSCCNC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1161328 10265 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Somatostatin receptor type 1 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 1 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1136 12 12 15 1.1 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)N(C(=O)c2ccccc2)C(=O)N(C)[C@H](O)NC(=O)[C@@H](N)CSSCCNC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
162651887 180271 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR1 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR1 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 180271 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR1 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR1 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
CHEMBL427658 213362 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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](Cc3ccc4ccccc4c3)C(=O)N2C)cc1 10.1021/jm049520l
CHEMBL411860 212961 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 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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(=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
CHEMBL264839 210631 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)N(C)C(=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
CHEMBL438630 213784 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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 213011 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 1.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 1.
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+
CHEMBL3349616 211442 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
44388119 160377 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1682 22 21 22 -1.7 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCC(=O)NCC[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
CHEMBL411109 160377 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1682 22 21 22 -1.7 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCC(=O)NCC[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
25189325 12446 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12446 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12446 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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
CHEMBL268448 210754 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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)N(C)C(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
11159133 115462 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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 115462 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1152 15 15 15 0.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
25189052 12672 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12672 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12672 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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
CHEMBL455760 214008 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst1 receptor expressed in CHOK1 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst1 receptor expressed in CHOK1 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
CHEMBL406373 212606 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity at human Somatostatin receptor type 1 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 1 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
44388109 161757 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1653 22 20 21 -0.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCCCC[C@@H](NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@@H]([C@@H](C)O)NC2=O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)O)CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc2ccccc2)C(=O)N3)cc1 10.1021/jm049519m
CHEMBL413924 161757 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 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1653 22 20 21 -0.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCCCC[C@@H](NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@@H]([C@@H](C)O)NC2=O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)O)CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc2ccccc2)C(=O)N3)cc1 10.1021/jm049519m
CHEMBL505128 214188 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptorDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptor
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
CHEMBL436962 213700 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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
CHEMBL3122128 211106 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[LTT]-SS28 from human SST1 receptor expressed in CHO cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST1 receptor expressed in CHO 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
CHEMBL414717 213150 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 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
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)cc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL408654 212726 0 None - 0 Human 8.1 pIC50 = 8.1 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 1.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 1.
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](CCCCNC(N)=O)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/jm010037+
42637632 60275 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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 60275 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
CHEMBL384855 212338 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 1Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3I)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(N)=O)CSSC[C@@H](N)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049520l
25187953 12689 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12689 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12689 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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
11457521 115459 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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 115459 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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
71460000 79659 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 1.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 1.
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 79659 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 1.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 1.
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+
44368406 10267 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Somatostatin receptor type 1 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 1 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1022 9 11 12 1.1 C[C@@H]1NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1161332 10267 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Somatostatin receptor type 1 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 1 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1022 9 11 12 1.1 C[C@@H]1NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350908 211527 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 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 12470 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12470 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12470 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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
16738359 137183 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 137183 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 137183 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 137183 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST1 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST1 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 137183 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST1 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST1 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 137183 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST1 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST1 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
CHEMBL440074 213859 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCCC[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)cc2I)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc2ccccc2)C(=O)N3)cc1 10.1021/jm049519m
44388107 159100 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1653 22 20 21 -0.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCCCC[C@H](NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@@H]([C@@H](C)O)NC2=O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)O)CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc2ccccc2)C(=O)N3)cc1 10.1021/jm049519m
CHEMBL409747 159100 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 1
ChEMBL 1653 22 20 21 -0.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCCCC[C@H](NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@@H]([C@@H](C)O)NC2=O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)O)CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc2ccccc2)C(=O)N3)cc1 10.1021/jm049519m
CHEMBL3349598 211427 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards cloned human somatostatin 1 (hsst) receptorBinding affinity towards cloned human somatostatin 1 (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
11642413 17100 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]iodotyrosyl from human SST1 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST1 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 17100 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]iodotyrosyl from human SST1 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST1 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
CHEMBL504087 214173 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptorDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptor
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
24777672 94912 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst1 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst1 receptor
ChEMBL 1027 18 12 11 1.0 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1 10.1021/jm070886i
CHEMBL254210 94912 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst1 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst1 receptor
ChEMBL 1027 18 12 11 1.0 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1 10.1021/jm070886i
25188496 12535 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12535 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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 12535 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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
42637137 195889 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
CHEMBL558935 195889 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst1 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
71460000 79659 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 1.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 1.
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 79659 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 1.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 1.
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+
CHEMBL3350890 211513 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
9849682 94952 0 None 8 10 Rat 9.7 pKd = 9.7 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 523 2 1 5 2.9 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL254500 94952 0 None 8 10 Rat 9.7 pKd = 9.7 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 523 2 1 5 2.9 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44441671 154984 0 None 23988 2 Rat 9.7 pKd = 9.7 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 542 4 0 10 1.8 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2Cc3c(cccc3OS(C)(=O)=O)C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL401290 154984 0 None 23988 2 Rat 9.7 pKd = 9.7 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 542 4 0 10 1.8 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2Cc3c(cccc3OS(C)(=O)=O)C[C@H]21 10.1016/j.bmcl.2007.04.086
44447075 94585 0 None 16218 2 Rat 9.6 pKd = 9.6 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 507 2 1 7 3.5 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252032 94585 0 None 16218 2 Rat 9.6 pKd = 9.6 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 507 2 1 7 3.5 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44447049 94954 0 None 93325 2 Rat 9.6 pKd = 9.6 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 537 3 1 5 3.4 CCn1c(N2CCN(C(=O)[C@@H]3C[C@@H]4c5cccc6[nH]c(Br)c(c56)C[C@H]4N(C)C3)CC2)cccc1=O 10.1016/j.bmcl.2007.12.030
CHEMBL254505 94954 0 None 93325 2 Rat 9.6 pKd = 9.6 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 537 3 1 5 3.4 CCn1c(N2CCN(C(=O)[C@@H]3C[C@@H]4c5cccc6[nH]c(Br)c(c56)C[C@H]4N(C)C3)CC2)cccc1=O 10.1016/j.bmcl.2007.12.030
2019 3675 0 None -4 10 Human 9.5 pKd = 9.5 Binding
Displacement of [125I]somatostatin from human SSTR1 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR1 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
44386062 3675 0 None -4 10 Human 9.5 pKd = 9.5 Binding
Displacement of [125I]somatostatin from human SSTR1 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR1 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
CHEMBL440072 3675 0 None -4 10 Human 9.5 pKd = 9.5 Binding
Displacement of [125I]somatostatin from human SSTR1 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR1 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
44565159 194891 0 None 6 5 Rat 9.5 pKd = 9.5 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 497 7 0 7 4.5 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL540705 194891 0 None 6 5 Rat 9.5 pKd = 9.5 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 497 7 0 7 4.5 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
44447073 94550 0 None 3 10 Rat 9.4 pKd = 9.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 534 2 1 6 3.8 CN1C[C@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL251835 94550 0 None 3 10 Rat 9.4 pKd = 9.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 534 2 1 6 3.8 CN1C[C@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44447076 94586 0 None 12302 2 Rat 9.4 pKd = 9.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 551 2 1 7 3.6 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252033 94586 0 None 12302 2 Rat 9.4 pKd = 9.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 551 2 1 7 3.6 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44447048 154988 0 None 31622 2 Rat 9.4 pKd = 9.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 493 3 1 5 3.3 CCn1c(N2CCN(C(=O)[C@@H]3C[C@@H]4c5cccc6[nH]c(Cl)c(c56)C[C@H]4N(C)C3)CC2)cccc1=O 10.1016/j.bmcl.2007.12.030
CHEMBL401309 154988 0 None 31622 2 Rat 9.4 pKd = 9.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 493 3 1 5 3.3 CCn1c(N2CCN(C(=O)[C@@H]3C[C@@H]4c5cccc6[nH]c(Cl)c(c56)C[C@H]4N(C)C3)CC2)cccc1=O 10.1016/j.bmcl.2007.12.030
44447045 94951 0 None 125892 2 Rat 9.4 pKd = 9.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 479 2 1 5 2.8 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL254499 94951 0 None 125892 2 Rat 9.4 pKd = 9.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 479 2 1 5 2.8 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44447071 154124 0 None 13182 2 Rat 9.4 pKd = 9.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 490 2 1 6 3.7 CN1C[C@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL398526 154124 0 None 13182 2 Rat 9.4 pKd = 9.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 490 2 1 6 3.7 CN1C[C@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44441673 94534 0 None 9772 2 Rat 9.4 pKd = 9.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 596 4 0 10 2.7 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2Cc3c(cccc3OS(=O)(=O)C(F)(F)F)C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL251754 94534 0 None 9772 2 Rat 9.4 pKd = 9.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 596 4 0 10 2.7 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2Cc3c(cccc3OS(=O)(=O)C(F)(F)F)C[C@H]21 10.1016/j.bmcl.2007.04.086
44441665 169133 0 None 9120 2 Rat 9.4 pKd = 9.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 528 5 0 8 2.3 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(cccc3OS(C)(=O)=O)C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL440236 169133 0 None 9120 2 Rat 9.4 pKd = 9.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 528 5 0 8 2.3 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(cccc3OS(C)(=O)=O)C[C@H]21 10.1016/j.bmcl.2007.04.086
44447038 94673 0 None 16595 2 Rat 9.3 pKd = 9.3 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 528 2 1 3 4.5 CN1C[C@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252618 94673 0 None 16595 2 Rat 9.3 pKd = 9.3 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 528 2 1 3 4.5 CN1C[C@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
10162564 12540 0 None 9 8 Rat 9.2 pKd = 9.2 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 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 12540 0 None 9 8 Rat 9.2 pKd = 9.2 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 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 12540 0 None 9 8 Rat 9.2 pKd = 9.2 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 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
44441672 94533 0 None 3311 2 Rat 9.2 pKd = 9.2 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 618 5 0 10 3.5 Cc1ccc(S(=O)(=O)Oc2cccc3c2C[C@H]2C[C@@H](C(=O)N4CCN(c5ccc6nsnc6n5)CC4)CN(C)[C@@H]2C3)cc1 10.1016/j.bmcl.2007.04.086
CHEMBL251753 94533 0 None 3311 2 Rat 9.2 pKd = 9.2 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 618 5 0 10 3.5 Cc1ccc(S(=O)(=O)Oc2cccc3c2C[C@H]2C[C@@H](C(=O)N4CCN(c5ccc6nsnc6n5)CC4)CN(C)[C@@H]2C3)cc1 10.1016/j.bmcl.2007.04.086
44447069 94644 0 None 21379 2 Rat 9.2 pKd = 9.2 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 484 2 1 3 4.4 CN1C[C@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252428 94644 0 None 21379 2 Rat 9.2 pKd = 9.2 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 484 2 1 3 4.4 CN1C[C@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44564783 176925 0 None 10 4 Rat 9.2 pKd = 9.2 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 484 8 0 5 4.8 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL461988 176925 0 None 10 4 Rat 9.2 pKd = 9.2 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 484 8 0 5 4.8 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
2030 3672 10 None 7 10 Rat 9.2 pKd = 9.2 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.078
5311377 3672 10 None 7 10 Rat 9.2 pKd = 9.2 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.078
CHEMBL251541 3672 10 None 7 10 Rat 9.2 pKd = 9.2 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.078
2030 3672 10 None 7 10 Rat 9.2 pKd = 9.2 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
5311377 3672 10 None 7 10 Rat 9.2 pKd = 9.2 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
CHEMBL251541 3672 10 None 7 10 Rat 9.2 pKd = 9.2 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
44565112 12759 0 None 3 6 Rat 9.1 pKd = 9.1 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1187847 12759 0 None 3 6 Rat 9.1 pKd = 9.1 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL523814 12759 0 None 3 6 Rat 9.1 pKd = 9.1 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44447043 94923 0 None 10232 2 Rat 9.1 pKd = 9.1 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 445 2 1 5 2.2 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL254288 94923 0 None 10232 2 Rat 9.1 pKd = 9.1 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 445 2 1 5 2.2 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
17955460 176775 0 None 2 9 Rat 9.1 pKd = 9.1 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 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 176775 0 None 2 9 Rat 9.1 pKd = 9.1 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 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
44441661 94492 0 None 7079 2 Rat 9.1 pKd = 9.1 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 492 5 0 6 3.8 CC(C)Oc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL251542 94492 0 None 7079 2 Rat 9.1 pKd = 9.1 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 492 5 0 6 3.8 CC(C)Oc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
44441678 94052 0 None 12022 2 Rat 9.1 pKd = 9.1 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 506 4 0 9 2.3 COc1ccc(C=O)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL248908 94052 0 None 12022 2 Rat 9.1 pKd = 9.1 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 506 4 0 9 2.3 COc1ccc(C=O)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
44564746 176961 0 None 7585 2 Rat 9.1 pKd = 9.1 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 500 8 0 6 4.9 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL462336 176961 0 None 7585 2 Rat 9.1 pKd = 9.1 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 500 8 0 6 4.9 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
44564815 189752 0 None 1905 2 Rat 9.0 pKd = 9.0 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 498 9 0 5 5.2 CCN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL515907 189752 0 None 1905 2 Rat 9.0 pKd = 9.0 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 498 9 0 5 5.2 CCN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44447042 94922 0 None 13489 2 Rat 9.0 pKd = 9.0 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 542 3 1 3 4.9 CCN1C[C@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL254287 94922 0 None 13489 2 Rat 9.0 pKd = 9.0 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 542 3 1 3 4.9 CCN1C[C@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44447074 94551 0 None 2951 2 Rat 9.0 pKd = 9.0 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 473 2 1 7 2.9 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL251836 94551 0 None 2951 2 Rat 9.0 pKd = 9.0 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 473 2 1 7 2.9 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44565114 12636 0 None - 1 Rat 9.0 pKd = 9.0 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 480 7 0 6 3.9 CN(CCC(=O)N1CCN(c2ccc3nccn3n2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1187144 12636 0 None - 1 Rat 9.0 pKd = 9.0 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 480 7 0 6 3.9 CN(CCC(=O)N1CCN(c2ccc3nccn3n2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL491497 12636 0 None - 1 Rat 9.0 pKd = 9.0 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 480 7 0 6 3.9 CN(CCC(=O)N1CCN(c2ccc3nccn3n2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44441677 94051 0 None 5248 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 556 3 0 8 3.2 COc1ccc(Br)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL248907 94051 0 None 5248 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 556 3 0 8 3.2 COc1ccc(Br)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
23656025 94094 0 None 8511 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 450 4 1 6 2.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL249113 94094 0 None 8511 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 450 4 1 6 2.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN[C@@H]1C2 10.1016/j.bmcl.2007.04.086
44441670 154644 0 None 3981 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 554 5 0 8 4.0 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2Cc3c(cccc3OCc3ccccc3)C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL399464 154644 0 None 3981 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 554 5 0 8 4.0 CN1C[C@H](C(=O)N2CCN(c3ccc4nsnc4n3)CC2)C[C@@H]2Cc3c(cccc3OCc3ccccc3)C[C@H]21 10.1016/j.bmcl.2007.04.086
44447073 94550 0 None -3 10 Human 8.9 pKd = 8.9 Binding
Binding affinity to human recombinant sst1 receptorBinding affinity to human recombinant sst1 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 94550 0 None -3 10 Human 8.9 pKd = 8.9 Binding
Binding affinity to human recombinant sst1 receptorBinding affinity to human recombinant sst1 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
44441669 94014 0 None 4677 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 478 3 0 8 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL248715 94014 0 None 4677 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 478 3 0 8 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441669 94014 0 None 4677 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 478 3 0 8 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL248715 94014 0 None 4677 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 478 3 0 8 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
44447064 154370 0 None 7079 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 493 3 1 5 4.0 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL398712 154370 0 None 7079 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 493 3 1 5 4.0 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44441899 154335 0 None 8511 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccc4[N+](=O)[O-])CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL398681 154335 0 None 8511 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccc4[N+](=O)[O-])CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441900 94300 0 None 5128 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc([N+](=O)[O-])c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250498 94300 0 None 5128 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc([N+](=O)[O-])c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44447066 94613 0 None 5370 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 537 3 1 5 4.1 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252229 94613 0 None 5370 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 537 3 1 5 4.1 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44441659 154680 0 None 7762 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 538 4 0 7 2.7 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2Cc3c(cccc3OS(=O)(=O)C(F)(F)F)C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL399658 154680 0 None 7762 2 Rat 8.9 pKd = 8.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 538 4 0 7 2.7 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2Cc3c(cccc3OS(=O)(=O)C(F)(F)F)C[C@H]21 10.1016/j.bmcl.2007.04.086
44441666 154720 0 None 2290 2 Rat 8.8 pKd = 8.8 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 582 5 0 8 3.2 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(cccc3OS(=O)(=O)C(F)(F)F)C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL399843 154720 0 None 2290 2 Rat 8.8 pKd = 8.8 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 582 5 0 8 3.2 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(cccc3OS(=O)(=O)C(F)(F)F)C[C@H]21 10.1016/j.bmcl.2007.04.086
17955460 176775 0 None -2 9 Human 8.8 pKd = 8.8 Binding
Binding affinity to human sst1 receptorBinding affinity to human sst1 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 176775 0 None -2 9 Human 8.8 pKd = 8.8 Binding
Binding affinity to human sst1 receptorBinding affinity to human sst1 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
44564859 12724 0 None - 1 Rat 8.8 pKd = 8.8 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 473 7 0 3 5.5 CN(CCC(=O)N1CCN(c2ccc(Cl)cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1187680 12724 0 None - 1 Rat 8.8 pKd = 8.8 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 473 7 0 3 5.5 CN(CCC(=O)N1CCN(c2ccc(Cl)cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL515113 12724 0 None - 1 Rat 8.8 pKd = 8.8 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 473 7 0 3 5.5 CN(CCC(=O)N1CCN(c2ccc(Cl)cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44441884 94393 0 None 2041 2 Rat 8.8 pKd = 8.8 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 461 3 0 7 2.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nonc5c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250922 94393 0 None 2041 2 Rat 8.8 pKd = 8.8 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 461 3 0 7 2.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nonc5c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
9849682 94952 0 None -8 10 Human 8.8 pKd = 8.8 Binding
Binding affinity to human recombinant sst1 receptorBinding affinity to human recombinant sst1 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 94952 0 None -8 10 Human 8.8 pKd = 8.8 Binding
Binding affinity to human recombinant sst1 receptorBinding affinity to human recombinant sst1 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
44441919 154770 0 None 3019 2 Rat 8.8 pKd = 8.8 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 542 5 0 8 2.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4S(C)(=O)=O)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL400137 154770 0 None 3019 2 Rat 8.8 pKd = 8.8 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 542 5 0 8 2.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4S(C)(=O)=O)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44564907 12532 0 None - 1 Rat 8.7 pKd = 8.7 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 507 7 0 3 6.2 CN(CCC(=O)N1CCN(c2ccc(Cl)c(Cl)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1186613 12532 0 None - 1 Rat 8.7 pKd = 8.7 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 507 7 0 3 6.2 CN(CCC(=O)N1CCN(c2ccc(Cl)c(Cl)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL472751 12532 0 None - 1 Rat 8.7 pKd = 8.7 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 507 7 0 3 6.2 CN(CCC(=O)N1CCN(c2ccc(Cl)c(Cl)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44565010 12638 0 None - 1 Rat 8.7 pKd = 8.7 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 457 7 0 3 5.0 CN(CCC(=O)N1CCN(c2ccc(F)cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1187146 12638 0 None - 1 Rat 8.7 pKd = 8.7 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 457 7 0 3 5.0 CN(CCC(=O)N1CCN(c2ccc(F)cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL491507 12638 0 None - 1 Rat 8.7 pKd = 8.7 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 457 7 0 3 5.0 CN(CCC(=O)N1CCN(c2ccc(F)cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44441897 94223 0 None 3715 2 Rat 8.7 pKd = 8.7 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 444 3 0 5 3.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccc4C#N)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL249930 94223 0 None 3715 2 Rat 8.7 pKd = 8.7 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 444 3 0 5 3.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccc4C#N)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
2030 3672 10 None -13 10 Human 8.0 pKd = 8.0 Binding
Binding affinity to human recombinant sst1 receptorBinding affinity to human recombinant sst1 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 3672 10 None -13 10 Human 8.0 pKd = 8.0 Binding
Binding affinity to human recombinant sst1 receptorBinding affinity to human recombinant sst1 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 3672 10 None -13 10 Human 8.0 pKd = 8.0 Binding
Binding affinity to human recombinant sst1 receptorBinding affinity to human recombinant sst1 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
44441886 154762 0 None 398 2 Rat 8.0 pKd = 8.0 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 477 3 0 7 3.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL400099 154762 0 None 398 2 Rat 8.0 pKd = 8.0 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 477 3 0 7 3.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
46880580 5547 0 None -346 2 Human 6.0 pKd = 6 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 5547 0 None -346 2 Human 6.0 pKd = 6 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
CHEMBL385409 212349 0 None -97 4 Human 6.0 pKd = 6 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)
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
CHEMBL437093 213705 0 None -16 5 Human 6.0 pKd = 6 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)
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
CHEMBL438471 213773 0 None -125 4 Human 6.0 pKd = 6 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)
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
46880574 6097 0 None -1 2 Human 7.0 pKd = 7.0 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 6097 0 None -1 2 Human 7.0 pKd = 7.0 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
44441871 94270 0 None 190 2 Rat 7.0 pKd = 7.0 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 488 3 0 5 3.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(F)(F)F)cn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250313 94270 0 None 190 2 Rat 7.0 pKd = 7.0 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 488 3 0 5 3.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(F)(F)F)cn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441873 94427 0 None 63 2 Rat 7.0 pKd = 7.0 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 526 6 0 6 4.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(OCc5ccccc5)n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL251116 94427 0 None 63 2 Rat 7.0 pKd = 7.0 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 526 6 0 6 4.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(OCc5ccccc5)n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441932 94461 0 None 4 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 343 2 1 4 1.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCNCC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL251301 94461 0 None 4 2 Rat 5.0 pKd = 5.0 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 343 2 1 4 1.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCNCC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441918 166871 0 None 44 2 Rat 7.0 pKd = 7.0 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 532 4 0 6 4.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(F)(F)F)cc4[N+](=O)[O-])CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL428583 166871 0 None 44 2 Rat 7.0 pKd = 7.0 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 532 4 0 6 4.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(F)(F)F)cc4[N+](=O)[O-])CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44564703 190497 0 None 446 2 Rat 7.9 pKd = 7.9 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 510 8 0 5 5.3 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2C=Cc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL517921 190497 0 None 446 2 Rat 7.9 pKd = 7.9 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 510 8 0 5 5.3 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2C=Cc2ccccc21 10.1016/j.bmcl.2009.01.072
44447029 171029 0 None - 1 Rat 5.9 pKd = 5.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 535 5 1 4 4.8 CCCCN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL445673 171029 0 None - 1 Rat 5.9 pKd = 5.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 535 5 1 4 4.8 CCCCN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
46865536 11919 0 None -151 7 Rat 5.9 pKd = 5.9 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST1 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST1 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 11919 0 None -151 7 Rat 5.9 pKd = 5.9 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST1 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST1 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 11919 0 None -151 7 Rat 5.9 pKd = 5.9 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST1 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST1 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
44564745 176960 0 None 478 2 Rat 7.9 pKd = 7.9 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 516 8 0 6 5.3 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL462335 176960 0 None 478 2 Rat 7.9 pKd = 7.9 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 516 8 0 6 5.3 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2009.01.072
44447009 94768 0 None - 1 Rat 7.9 pKd = 7.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 449 2 1 4 3.5 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL253234 94768 0 None - 1 Rat 7.9 pKd = 7.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 449 2 1 4 3.5 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
46880573 6096 0 None -1 2 Human 6.9 pKd = 6.9 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 6096 0 None -1 2 Human 6.9 pKd = 6.9 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
CHEMBL407209 212647 1 None -1949 4 Human 5.9 pKd = 5.9 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)
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
CHEMBL384836 212337 0 None -74 5 Human 5.9 pKd = 5.9 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)
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
44564814 180037 0 None 602 2 Rat 7.9 pKd = 7.9 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 486 10 0 5 4.8 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.01.072
CHEMBL474752 180037 0 None 602 2 Rat 7.9 pKd = 7.9 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 486 10 0 5 4.8 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.01.072
44441680 94093 0 None 11 2 Rat 5.9 pKd = 5.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@@H]1C[C@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL249112 94093 0 None 11 2 Rat 5.9 pKd = 5.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@@H]1C[C@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL2370166 209805 0 None -977 5 Human 4.9 pKd = 4.9 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst1) expressed in hSF6 cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst1) expressed in hSF6 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
46865535 5539 0 None -407 7 Human 5.9 pKd = 5.9 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 5539 0 None -407 7 Human 5.9 pKd = 5.9 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
44447006 94766 0 None 1258 2 Rat 7.9 pKd = 7.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 415 2 1 4 2.9 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL253232 94766 0 None 1258 2 Rat 7.9 pKd = 7.9 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 415 2 1 4 2.9 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44447034 154757 0 None - 1 Rat 5.8 pKd = 5.8 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 537 5 1 5 3.7 COCCN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL400066 154757 0 None - 1 Rat 5.8 pKd = 5.8 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 537 5 1 5 3.7 COCCN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44441667 154941 0 None 457 2 Rat 7.8 pKd = 7.8 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 459 3 0 6 2.9 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(C#N)cccc3C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL401091 154941 0 None 457 2 Rat 7.8 pKd = 7.8 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 459 3 0 6 2.9 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(C#N)cccc3C[C@H]21 10.1016/j.bmcl.2007.04.086
44441906 94351 0 None 57 2 Rat 6.8 pKd = 6.8 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 461 4 0 5 3.3 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(C)=O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250705 94351 0 None 57 2 Rat 6.8 pKd = 6.8 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 461 4 0 5 3.3 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(C)=O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441909 94221 0 None 10 2 Rat 5.8 pKd = 5.8 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 462 4 1 5 2.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(N)=O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL249892 94221 0 None 10 2 Rat 5.8 pKd = 5.8 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 462 4 1 5 2.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(N)=O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
46865536 11919 0 None -199 7 Human 5.8 pKd = 5.8 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 11919 0 None -199 7 Human 5.8 pKd = 5.8 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 11919 0 None -199 7 Human 5.8 pKd = 5.8 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
44441660 94465 0 None 204 2 Rat 6.8 pKd = 6.8 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 390 2 0 4 2.5 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2Cc3ccccc3C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL251335 94465 0 None 204 2 Rat 6.8 pKd = 6.8 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 390 2 0 4 2.5 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2Cc3ccccc3C[C@H]21 10.1016/j.bmcl.2007.04.086
44447014 94829 0 None 338 2 Rat 7.8 pKd = 7.8 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 541 2 1 4 3.5 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(I)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL253653 94829 0 None 338 2 Rat 7.8 pKd = 7.8 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 541 2 1 4 3.5 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(I)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44441908 94388 0 None 91 2 Rat 6.8 pKd = 6.8 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 477 4 0 6 2.9 COC(=O)c1ccc(N2CCN(C(=O)[C@@H]3C[C@@H]4Cc5c(cccc5OC)C[C@H]4N(C)C3)CC2)cc1 10.1016/j.bmcl.2007.04.078
CHEMBL250900 94388 0 None 91 2 Rat 6.8 pKd = 6.8 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 477 4 0 6 2.9 COC(=O)c1ccc(N2CCN(C(=O)[C@@H]3C[C@@H]4Cc5c(cccc5OC)C[C@H]4N(C)C3)CC2)cc1 10.1016/j.bmcl.2007.04.078
46880853 5565 0 None -147 2 Human 5.8 pKd = 5.8 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 5565 0 None -147 2 Human 5.8 pKd = 5.8 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
44447026 94580 0 None 46 2 Rat 6.8 pKd = 6.8 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 479 2 2 4 3.3 O=C([C@H]1CN[C@@H]2Cc3c(Br)[nH]c4cccc(c34)[C@H]2C1)N1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2007.12.030
CHEMBL252002 94580 0 None 46 2 Rat 6.8 pKd = 6.8 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 479 2 2 4 3.3 O=C([C@H]1CN[C@@H]2Cc3c(Br)[nH]c4cccc(c34)[C@H]2C1)N1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2007.12.030
44441910 94222 0 None 11 2 Rat 5.8 pKd = 5.8 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 518 6 0 5 3.6 CCN(CC)C(=O)c1ccc(N2CCN(C(=O)[C@@H]3C[C@@H]4Cc5c(cccc5OC)C[C@H]4N(C)C3)CC2)cc1 10.1016/j.bmcl.2007.04.078
CHEMBL249893 94222 0 None 11 2 Rat 5.8 pKd = 5.8 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 518 6 0 5 3.6 CCN(CC)C(=O)c1ccc(N2CCN(C(=O)[C@@H]3C[C@@H]4Cc5c(cccc5OC)C[C@H]4N(C)C3)CC2)cc1 10.1016/j.bmcl.2007.04.078
44441658 94464 0 None 588 2 Rat 7.8 pKd = 7.8 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 420 3 0 5 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL251334 94464 0 None 588 2 Rat 7.8 pKd = 7.8 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 420 3 0 5 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441658 94464 0 None 588 2 Rat 7.8 pKd = 7.8 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 420 3 0 5 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL251334 94464 0 None 588 2 Rat 7.8 pKd = 7.8 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 420 3 0 5 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
44564903 12550 0 None - 1 Rat 7.8 pKd = 7.8 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 473 7 0 3 5.5 CN(CCC(=O)N1CCN(c2cccc(Cl)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1186691 12550 0 None - 1 Rat 7.8 pKd = 7.8 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 473 7 0 3 5.5 CN(CCC(=O)N1CCN(c2cccc(Cl)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL474745 12550 0 None - 1 Rat 7.8 pKd = 7.8 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 473 7 0 3 5.5 CN(CCC(=O)N1CCN(c2cccc(Cl)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44441890 94462 0 None 1047 2 Rat 7.8 pKd = 7.8 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 437 3 0 4 3.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccc4F)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL251311 94462 0 None 1047 2 Rat 7.8 pKd = 7.8 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 437 3 0 4 3.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccccc4F)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44447032 94866 0 None - 1 Rat 5.8 pKd = 5.8 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 549 5 1 4 5.1 CC(C)CCN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL253880 94866 0 None - 1 Rat 5.8 pKd = 5.8 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 549 5 1 4 5.1 CC(C)CCN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44564702 189868 0 None 190 2 Rat 7.7 pKd = 7.7 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 512 8 0 5 4.9 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2CCc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL516837 189868 0 None 190 2 Rat 7.7 pKd = 7.7 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 512 8 0 5 4.9 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2CCc2ccccc21 10.1016/j.bmcl.2009.01.072
44441662 94493 0 None 416 2 Rat 7.7 pKd = 7.7 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 450 3 1 6 2.7 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL251543 94493 0 None 416 2 Rat 7.7 pKd = 7.7 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 450 3 1 6 2.7 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmcl.2007.04.086
44447078 94617 0 None 2 7 Rat 6.7 pKd = 6.7 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 534 2 1 6 3.8 CN1C[C@@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@H]2c3cccc4[nH]c(Br)c(c34)C[C@@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252232 94617 0 None 2 7 Rat 6.7 pKd = 6.7 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 534 2 1 6 3.8 CN1C[C@@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@H]2c3cccc4[nH]c(Br)c(c34)C[C@@H]21 10.1016/j.bmcl.2007.12.030
44441867 94245 0 None 9 2 Rat 5.7 pKd = 5.7 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 420 3 0 5 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccncc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250111 94245 0 None 9 2 Rat 5.7 pKd = 5.7 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 420 3 0 5 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccncc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44447052 154951 0 None 112 2 Rat 7.7 pKd = 7.7 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 448 2 1 3 4.1 CN1C[C@H](C(=O)N2CCN(c3ccc(Cl)cc3)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL401130 154951 0 None 112 2 Rat 7.7 pKd = 7.7 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 448 2 1 3 4.1 CN1C[C@H](C(=O)N2CCN(c3ccc(Cl)cc3)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
46880856 5561 0 None -66 2 Human 5.7 pKd = 5.7 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 5561 0 None -66 2 Human 5.7 pKd = 5.7 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
44447077 94616 0 None -4 7 Human 5.7 pKd = 5.7 Binding
Binding affinity to human recombinant sst1 receptorBinding affinity to human recombinant sst1 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 94616 0 None -4 7 Human 5.7 pKd = 5.7 Binding
Binding affinity to human recombinant sst1 receptorBinding affinity to human recombinant sst1 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
44565159 194891 0 None -6 5 Human 8.7 pKd = 8.7 Binding
Binding affinity to human sst1 receptorBinding affinity to human sst1 receptor
ChEMBL 497 7 0 7 4.5 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL540705 194891 0 None -6 5 Human 8.7 pKd = 8.7 Binding
Binding affinity to human sst1 receptorBinding affinity to human sst1 receptor
ChEMBL 497 7 0 7 4.5 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
44565064 12633 0 None - 1 Rat 8.7 pKd = 8.7 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 470 7 0 5 3.6 CN(CCC(=O)N1CCN(c2cccc(=O)n2C)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1187127 12633 0 None - 1 Rat 8.7 pKd = 8.7 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 470 7 0 5 3.6 CN(CCC(=O)N1CCN(c2cccc(=O)n2C)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL491144 12633 0 None - 1 Rat 8.7 pKd = 8.7 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 470 7 0 5 3.6 CN(CCC(=O)N1CCN(c2cccc(=O)n2C)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44447019 94865 0 None 3548 2 Rat 8.6 pKd = 8.6 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 461 3 1 5 3.6 CSc1[nH]c2cccc3c2c1C[C@@H]1[C@@H]3C[C@@H](C(=O)N2CCN(c3ccccn3)CC2)CN1C 10.1016/j.bmcl.2007.12.030
CHEMBL253879 94865 0 None 3548 2 Rat 8.6 pKd = 8.6 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 461 3 1 5 3.6 CSc1[nH]c2cccc3c2c1C[C@@H]1[C@@H]3C[C@@H](C(=O)N2CCN(c3ccccn3)CC2)CN1C 10.1016/j.bmcl.2007.12.030
44565112 12759 0 None -3 6 Human 8.6 pKd = 8.6 Binding
Binding affinity to human sst1 receptorBinding affinity to human sst1 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1187847 12759 0 None -3 6 Human 8.6 pKd = 8.6 Binding
Binding affinity to human sst1 receptorBinding affinity to human sst1 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL523814 12759 0 None -3 6 Human 8.6 pKd = 8.6 Binding
Binding affinity to human sst1 receptorBinding affinity to human sst1 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44441885 94428 0 None 3630 2 Rat 8.6 pKd = 8.6 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 477 3 0 7 3.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc5nsnc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL251120 94428 0 None 3630 2 Rat 8.6 pKd = 8.6 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 477 3 0 7 3.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc5nsnc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
23656026 94266 0 None -3 2 Rat 8.6 pKd = 8.6 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 455 3 0 4 3.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250304 94266 0 None -3 2 Rat 8.6 pKd = 8.6 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 455 3 0 4 3.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441916 154769 0 None 5888 2 Rat 8.6 pKd = 8.6 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 462 3 0 5 3.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(F)c4C#N)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL400136 154769 0 None 5888 2 Rat 8.6 pKd = 8.6 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 462 3 0 5 3.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(F)c4C#N)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
9871544 14216 3 None -416 11 Human 5.7 pKd = 5.7 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 14216 3 None -416 11 Human 5.7 pKd = 5.7 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 14216 3 None -416 11 Human 5.7 pKd = 5.7 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
44441921 94352 0 None 165 2 Rat 6.7 pKd = 6.7 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 434 3 0 5 2.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCCN(c4ccccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250713 94352 0 None 165 2 Rat 6.7 pKd = 6.7 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 434 3 0 5 2.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCCN(c4ccccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44565068 12748 0 None - 1 Rat 7.7 pKd = 7.7 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 440 7 0 4 4.3 CN(CCC(=O)N1CCN(c2ccncc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1187808 12748 0 None - 1 Rat 7.7 pKd = 7.7 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 440 7 0 4 4.3 CN(CCC(=O)N1CCN(c2ccncc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL522135 12748 0 None - 1 Rat 7.7 pKd = 7.7 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 440 7 0 4 4.3 CN(CCC(=O)N1CCN(c2ccncc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44441902 154875 0 None 562 2 Rat 7.6 pKd = 7.6 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 487 3 0 4 4.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(C(F)(F)F)c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL400709 154875 0 None 562 2 Rat 7.6 pKd = 7.6 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 487 3 0 4 4.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(C(F)(F)F)c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44564905 12531 0 None - 1 Rat 7.6 pKd = 7.6 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 473 7 0 3 5.5 CN(CCC(=O)N1CCN(c2ccccc2Cl)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1186612 12531 0 None - 1 Rat 7.6 pKd = 7.6 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 473 7 0 3 5.5 CN(CCC(=O)N1CCN(c2ccccc2Cl)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL472750 12531 0 None - 1 Rat 7.6 pKd = 7.6 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 473 7 0 3 5.5 CN(CCC(=O)N1CCN(c2ccccc2Cl)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
46880581 5548 0 None -21 2 Human 5.6 pKd = 5.6 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 5548 0 None -21 2 Human 5.6 pKd = 5.6 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
46880855 5560 0 None -165 2 Human 5.6 pKd = 5.6 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 5560 0 None -165 2 Human 5.6 pKd = 5.6 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
44447037 94672 0 None - 1 Rat 5.6 pKd = 5.6 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 537 5 2 5 3.4 O=C([C@@H]1C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]2N(CCCO)C1)N1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2007.12.030
CHEMBL252617 94672 0 None - 1 Rat 5.6 pKd = 5.6 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 537 5 2 5 3.4 O=C([C@@H]1C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]2N(CCCO)C1)N1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2007.12.030
44447016 94830 0 None 35 2 Rat 6.6 pKd = 6.6 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 431 2 2 5 2.6 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(O)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL253654 94830 0 None 35 2 Rat 6.6 pKd = 6.6 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 431 2 2 5 2.6 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(O)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
46880576 5543 0 None -1 2 Human 5.6 pKd = 5.6 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 5543 0 None -1 2 Human 5.6 pKd = 5.6 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
44441663 94491 0 None 660 2 Rat 7.6 pKd = 7.6 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 534 4 0 7 3.9 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(cccc3OC(=O)C(C)(C)C)C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL251529 94491 0 None 660 2 Rat 7.6 pKd = 7.6 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 534 4 0 7 3.9 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(cccc3OC(=O)C(C)(C)C)C[C@H]21 10.1016/j.bmcl.2007.04.086
44441923 94353 0 None 85 2 Rat 6.6 pKd = 6.6 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 478 4 0 6 3.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250715 94353 0 None 85 2 Rat 6.6 pKd = 6.6 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 478 4 0 6 3.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
20597810 5559 0 None -245 2 Human 5.6 pKd = 5.6 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 5559 0 None -245 2 Human 5.6 pKd = 5.6 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
44447023 94545 0 None 6 2 Rat 5.6 pKd = 5.6 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 477 3 1 5 2.6 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c([S+](C)[O-])c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL251801 94545 0 None 6 2 Rat 5.6 pKd = 5.6 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 477 3 1 5 2.6 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c([S+](C)[O-])c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44441879 94356 0 None 75 2 Rat 7.6 pKd = 7.6 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 470 3 0 5 3.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5ccccc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250724 94356 0 None 75 2 Rat 7.6 pKd = 7.6 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 470 3 0 5 3.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5ccccc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44564786 176816 0 None 60 2 Rat 6.6 pKd = 6.6 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 446 8 0 5 4.0 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCc1ccc2ccccc2c1 10.1016/j.bmcl.2009.01.072
CHEMBL460934 176816 0 None 60 2 Rat 6.6 pKd = 6.6 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 446 8 0 5 4.0 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCc1ccc2ccccc2c1 10.1016/j.bmcl.2009.01.072
44441903 94349 0 None 18 2 Rat 6.6 pKd = 6.6 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 487 3 0 4 4.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(F)(F)F)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250703 94349 0 None 18 2 Rat 6.6 pKd = 6.6 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 487 3 0 4 4.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(F)(F)F)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441880 169227 0 None 19 2 Rat 6.5 pKd = 6.5 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 470 3 0 5 3.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cc5ccccc5cn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL440962 169227 0 None 19 2 Rat 6.5 pKd = 6.5 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 470 3 0 5 3.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cc5ccccc5cn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44564744 176943 0 None 630 2 Rat 7.5 pKd = 7.5 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 498 8 0 5 4.7 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2Cc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL462159 176943 0 None 630 2 Rat 7.5 pKd = 7.5 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 498 8 0 5 4.7 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2Cc2ccccc21 10.1016/j.bmcl.2009.01.072
44441917 94267 0 None 1348 2 Rat 8.5 pKd = 8.5 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 489 4 0 7 2.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4C#N)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250305 94267 0 None 1348 2 Rat 8.5 pKd = 8.5 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 489 4 0 7 2.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4C#N)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44564949 12539 0 None - 1 Rat 8.5 pKd = 8.5 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)cc2F)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1186651 12539 0 None - 1 Rat 8.5 pKd = 8.5 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)cc2F)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL473762 12539 0 None - 1 Rat 8.5 pKd = 8.5 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)cc2F)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44441893 94193 0 None 6456 2 Rat 8.5 pKd = 8.5 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 437 3 0 4 3.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(F)c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL249723 94193 0 None 6456 2 Rat 8.5 pKd = 8.5 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 437 3 0 4 3.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(F)c4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441894 154911 0 None 7762 2 Rat 8.5 pKd = 8.5 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 437 3 0 4 3.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(F)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL400907 154911 0 None 7762 2 Rat 8.5 pKd = 8.5 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 437 3 0 4 3.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(F)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441870 169131 0 None 2884 2 Rat 8.5 pKd = 8.5 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 445 3 0 6 2.3 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C#N)cn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL440233 169131 0 None 2884 2 Rat 8.5 pKd = 8.5 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 445 3 0 6 2.3 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C#N)cn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441674 154617 0 None 3890 2 Rat 8.5 pKd = 8.5 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 498 4 0 6 3.6 COc1ccc(Cl)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL399267 154617 0 None 3890 2 Rat 8.5 pKd = 8.5 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 498 4 0 6 3.6 COc1ccc(Cl)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
44564909 12533 0 None - 1 Rat 8.4 pKd = 8.4 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 457 7 0 3 5.0 CN(CCC(=O)N1CCN(c2cccc(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1186614 12533 0 None - 1 Rat 8.4 pKd = 8.4 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 457 7 0 3 5.0 CN(CCC(=O)N1CCN(c2cccc(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL472752 12533 0 None - 1 Rat 8.4 pKd = 8.4 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 457 7 0 3 5.0 CN(CCC(=O)N1CCN(c2cccc(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44441883 94392 0 None 999 2 Rat 8.4 pKd = 8.4 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 461 3 0 7 2.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc5nonc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250921 94392 0 None 999 2 Rat 8.4 pKd = 8.4 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 461 3 0 7 2.6 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc5nonc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44447062 94582 0 None 812 2 Rat 8.4 pKd = 8.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 459 3 1 5 3.4 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252029 94582 0 None 812 2 Rat 8.4 pKd = 8.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 459 3 1 5 3.4 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44441926 94390 0 None 77 2 Rat 7.5 pKd = 7.5 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 417 3 0 4 3.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CC=C(c4ccccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250914 94390 0 None 77 2 Rat 7.5 pKd = 7.5 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 417 3 0 4 3.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CC=C(c4ccccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44447025 154947 0 None 25 2 Rat 6.5 pKd = 6.5 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 493 3 1 6 2.3 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(S(C)(=O)=O)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL401108 154947 0 None 25 2 Rat 6.5 pKd = 6.5 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 493 3 1 6 2.3 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(S(C)(=O)=O)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44564952 12516 0 None - 1 Rat 7.5 pKd = 7.5 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 507 7 0 3 5.9 CN(CCC(=O)N1CCN(c2ccc(C(F)(F)F)cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1186578 12516 0 None - 1 Rat 7.5 pKd = 7.5 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 507 7 0 3 5.9 CN(CCC(=O)N1CCN(c2ccc(C(F)(F)F)cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL470500 12516 0 None - 1 Rat 7.5 pKd = 7.5 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 507 7 0 3 5.9 CN(CCC(=O)N1CCN(c2ccc(C(F)(F)F)cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
155544425 173382 0 None -14125 5 Human 6.5 pKd = 6.5 Binding
Displacement of [125I]somatostatin from human SSTR1 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR1 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 173382 0 None -14125 5 Human 6.5 pKd = 6.5 Binding
Displacement of [125I]somatostatin from human SSTR1 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR1 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
CHEMBL407571 212669 0 None -309 4 Human 6.5 pKd = 6.5 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)
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
44564784 176941 0 None 43 2 Rat 6.5 pKd = 6.5 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 485 8 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCn1c2ccccc2c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL462157 176941 0 None 43 2 Rat 6.5 pKd = 6.5 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 485 8 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCn1c2ccccc2c2ccccc21 10.1016/j.bmcl.2009.01.072
44441679 94092 0 None 83 2 Rat 7.5 pKd = 7.5 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 520 4 0 9 2.7 COc1ccc(C(C)=O)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL249111 94092 0 None 83 2 Rat 7.5 pKd = 7.5 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 520 4 0 9 2.7 COc1ccc(C(C)=O)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nsnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
44441882 94391 0 None 19 2 Rat 6.5 pKd = 6.5 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 472 3 0 7 2.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cc5nccnc5cn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250920 94391 0 None 19 2 Rat 6.5 pKd = 6.5 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 472 3 0 7 2.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cc5nccnc5cn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL2370167 209806 0 None -1621 5 Human 5.5 pKd = 5.5 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst1) expressed in hSF6 cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst1) expressed in hSF6 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
CHEMBL405421 212560 0 None -363 4 Human 6.4 pKd = 6.4 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)
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
46880590 5540 0 None 2 2 Human 7.4 pKd = 7.4 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 5540 0 None 2 2 Human 7.4 pKd = 7.4 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
46880582 5549 0 None -295 2 Human 6.4 pKd = 6.4 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 5549 0 None -295 2 Human 6.4 pKd = 6.4 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
44447058 154952 0 None 1412 2 Rat 8.4 pKd = 8.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 482 2 1 3 4.8 CN1C[C@H](C(=O)N2CCN(c3ccc(Cl)cc3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL401131 154952 0 None 1412 2 Rat 8.4 pKd = 8.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 482 2 1 3 4.8 CN1C[C@H](C(=O)N2CCN(c3ccc(Cl)cc3)CC2)C[C@@H]2c3cccc4[nH]c(Cl)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44447011 94798 0 None 3715 2 Rat 8.4 pKd = 8.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 493 2 1 4 3.6 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL253438 94798 0 None 3715 2 Rat 8.4 pKd = 8.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 493 2 1 4 3.6 CN1C[C@H](C(=O)N2CCN(c3ccccn3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44565116 12637 0 None - 1 Rat 8.3 pKd = 8.3 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 483 7 0 5 4.6 CN(CCC(=O)N1CCN(c2ccc3c(c2)OCO3)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1187145 12637 0 None - 1 Rat 8.3 pKd = 8.3 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 483 7 0 5 4.6 CN(CCC(=O)N1CCN(c2ccc3c(c2)OCO3)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL491498 12637 0 None - 1 Rat 8.3 pKd = 8.3 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 483 7 0 5 4.6 CN(CCC(=O)N1CCN(c2ccc3c(c2)OCO3)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44565012 12639 0 None - 1 Rat 8.3 pKd = 8.3 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 464 7 0 4 4.7 CN(CCC(=O)N1CCN(c2ccccc2C#N)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1187147 12639 0 None - 1 Rat 8.3 pKd = 8.3 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 464 7 0 4 4.7 CN(CCC(=O)N1CCN(c2ccccc2C#N)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL491508 12639 0 None - 1 Rat 8.3 pKd = 8.3 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 464 7 0 4 4.7 CN(CCC(=O)N1CCN(c2ccccc2C#N)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44441675 94015 0 None 1995 2 Rat 8.3 pKd = 8.3 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 542 4 0 6 3.8 COc1ccc(Br)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL248716 94015 0 None 1995 2 Rat 8.3 pKd = 8.3 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 542 4 0 6 3.8 COc1ccc(Br)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
44564816 189513 0 None 194 2 Rat 8.3 pKd = 8.3 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 512 9 0 5 5.5 CC(C)N(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL514027 189513 0 None 194 2 Rat 8.3 pKd = 8.3 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 512 9 0 5 5.5 CC(C)N(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44441664 94531 0 None 3235 2 Rat 8.3 pKd = 8.3 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 550 4 0 8 4.3 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(cccc3OC(=O)OC(C)(C)C)C[C@H]21 10.1016/j.bmcl.2007.04.086
CHEMBL251751 94531 0 None 3235 2 Rat 8.3 pKd = 8.3 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 550 4 0 8 4.3 CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2Cc3c(cccc3OC(=O)OC(C)(C)C)C[C@H]21 10.1016/j.bmcl.2007.04.086
44447077 94616 0 None 4 7 Rat 6.4 pKd = 6.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 523 2 1 5 2.9 CN1C[C@@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@H]2c3cccc4[nH]c(Br)c(c34)C[C@@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252231 94616 0 None 4 7 Rat 6.4 pKd = 6.4 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 523 2 1 5 2.9 CN1C[C@@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@H]2c3cccc4[nH]c(Br)c(c34)C[C@@H]21 10.1016/j.bmcl.2007.12.030
46880583 5537 0 None -194 2 Human 6.4 pKd = 6.4 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 5537 0 None -194 2 Human 6.4 pKd = 6.4 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
44564857 178938 0 None 1 4 Rat 7.3 pKd = 7.3 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 524 10 0 5 5.5 O=C(CCN(CCC1c2ccccc2-c2ccccc21)CC1CC1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.bmcl.2009.01.072
CHEMBL470331 178938 0 None 1 4 Rat 7.3 pKd = 7.3 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 524 10 0 5 5.5 O=C(CCN(CCC1c2ccccc2-c2ccccc21)CC1CC1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.bmcl.2009.01.072
46865535 5539 0 None -134 7 Rat 6.3 pKd = 6.3 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST1 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST1 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 5539 0 None -134 7 Rat 6.3 pKd = 6.3 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST1 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST1 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
44441931 154822 0 None 19 2 Rat 6.3 pKd = 6.3 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 433 4 0 4 3.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(Cc4ccccc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL400386 154822 0 None 19 2 Rat 6.3 pKd = 6.3 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 433 4 0 4 3.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(Cc4ccccc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL421362 213274 0 None -1258 5 Human 5.3 pKd = 5.3 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst1) expressed in hSF6 cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst1) expressed in hSF6 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
44441869 154870 0 None 58 2 Rat 6.3 pKd = 6.3 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 421 3 0 6 1.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ncccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL400677 154870 0 None 58 2 Rat 6.3 pKd = 6.3 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 421 3 0 6 1.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ncccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
46880575 5542 0 None -3 2 Human 6.3 pKd = 6.3 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 5542 0 None -3 2 Human 6.3 pKd = 6.3 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
44441927 94425 0 None 4 2 Rat 6.3 pKd = 6.3 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 418 3 0 5 2.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CC=C(c4ncccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL251110 94425 0 None 4 2 Rat 6.3 pKd = 6.3 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 418 3 0 5 2.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CC=C(c4ncccn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441928 94426 0 None 4 2 Rat 6.3 pKd = 6.3 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 474 3 1 5 3.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCC(n4c(=O)[nH]c5ccccc54)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL251111 94426 0 None 4 2 Rat 6.3 pKd = 6.3 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 474 3 1 5 3.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCC(n4c(=O)[nH]c5ccccc54)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
10162564 12540 0 None -9 8 Human 8.3 pKd = 8.3 Binding
Binding affinity to human sst1 receptorBinding affinity to human sst1 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 12540 0 None -9 8 Human 8.3 pKd = 8.3 Binding
Binding affinity to human sst1 receptorBinding affinity to human sst1 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 12540 0 None -9 8 Human 8.3 pKd = 8.3 Binding
Binding affinity to human sst1 receptorBinding affinity to human sst1 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
44447060 194831 0 None 363 2 Rat 8.3 pKd = 8.3 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 526 2 1 3 4.9 CN1C[C@H](C(=O)N2CCN(c3ccc(Cl)cc3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL539415 194831 0 None 363 2 Rat 8.3 pKd = 8.3 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat cortexDisplacement of [125I]SRIF14 from sst1 receptor in rat cortex
ChEMBL 526 2 1 3 4.9 CN1C[C@H](C(=O)N2CCN(c3ccc(Cl)cc3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
44441881 154290 0 None 2454 2 Rat 8.2 pKd = 8.2 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 472 3 0 7 2.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nccnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL398656 154290 0 None 2454 2 Rat 8.2 pKd = 8.2 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 472 3 0 7 2.4 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nccnc5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44447078 94617 0 None -2 7 Human 6.3 pKd = 6.3 Binding
Binding affinity to human recombinant sst1 receptorBinding affinity to human recombinant sst1 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 94617 0 None -2 7 Human 6.3 pKd = 6.3 Binding
Binding affinity to human recombinant sst1 receptorBinding affinity to human recombinant sst1 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
44441868 154840 0 None 478 2 Rat 7.3 pKd = 7.3 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 421 3 0 6 1.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccnn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL400481 154840 0 None 478 2 Rat 7.3 pKd = 7.3 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 421 3 0 6 1.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccnn4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
46880577 5544 0 None -3 2 Human 6.3 pKd = 6.3 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 5544 0 None -3 2 Human 6.3 pKd = 6.3 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
44441872 94271 0 None 18 2 Rat 6.3 pKd = 6.3 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 568 5 0 8 2.7 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ncccc4OS(=O)(=O)C(F)(F)F)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250314 94271 0 None 18 2 Rat 6.3 pKd = 6.3 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 568 5 0 8 2.7 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ncccc4OS(=O)(=O)C(F)(F)F)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
9871544 14216 3 None -120 11 Rat 6.2 pKd = 6.2 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST1 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST1 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 14216 3 None -120 11 Rat 6.2 pKd = 6.2 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST1 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST1 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 14216 3 None -120 11 Rat 6.2 pKd = 6.2 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST1 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST1 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
44441914 153903 0 None 15 2 Rat 6.2 pKd = 6.2 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 498 4 1 6 1.7 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(S(N)(=O)=O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL398319 153903 0 None 15 2 Rat 6.2 pKd = 6.2 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 498 4 1 6 1.7 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(S(N)(=O)=O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441668 94532 0 None 1202 2 Rat 8.2 pKd = 8.2 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 476 4 0 6 3.2 CC(=O)c1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL251752 94532 0 None 1202 2 Rat 8.2 pKd = 8.2 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 476 4 0 6 3.2 CC(=O)c1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
44565066 12634 0 None - 1 Rat 8.2 pKd = 8.2 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 471 7 0 6 3.0 CN(CCC(=O)N1CCN(c2ccc(=O)n(C)n2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1187128 12634 0 None - 1 Rat 8.2 pKd = 8.2 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 471 7 0 6 3.0 CN(CCC(=O)N1CCN(c2ccc(=O)n(C)n2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL491145 12634 0 None - 1 Rat 8.2 pKd = 8.2 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 471 7 0 6 3.0 CN(CCC(=O)N1CCN(c2ccc(=O)n(C)n2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44565008 12667 0 None - 1 Rat 7.2 pKd = 7.2 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 507 7 0 3 5.9 CN(CCC(=O)N1CCN(c2cccc(C(F)(F)F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1187261 12667 0 None - 1 Rat 7.2 pKd = 7.2 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 507 7 0 3 5.9 CN(CCC(=O)N1CCN(c2cccc(C(F)(F)F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL495264 12667 0 None - 1 Rat 7.2 pKd = 7.2 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 507 7 0 3 5.9 CN(CCC(=O)N1CCN(c2cccc(C(F)(F)F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL413830 213089 0 None -23 5 Human 6.2 pKd = 6.2 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)
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
46880579 5546 0 None -5 2 Human 5.2 pKd = 5.2 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 5546 0 None -5 2 Human 5.2 pKd = 5.2 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
CHEMBL409019 212742 0 None -21 5 Human 6.2 pKd = 6.2 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)
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
44441913 94244 0 None 13 2 Rat 6.2 pKd = 6.2 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 497 4 0 6 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(S(C)(=O)=O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250098 94244 0 None 13 2 Rat 6.2 pKd = 6.2 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 497 4 0 6 2.5 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(S(C)(=O)=O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441905 94350 0 None 38 2 Rat 6.2 pKd = 6.2 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 435 3 1 5 2.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250704 94350 0 None 38 2 Rat 6.2 pKd = 6.2 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 435 3 1 5 2.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL386676 212386 0 None -16 4 Human 6.2 pKd = 6.2 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)
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
44441878 94355 0 None 7 2 Rat 6.2 pKd = 6.2 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 484 3 0 5 3.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cc(C)nc5ccccc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250723 94355 0 None 7 2 Rat 6.2 pKd = 6.2 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 484 3 0 5 3.9 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cc(C)nc5ccccc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44564856 179672 0 None 575 2 Rat 8.2 pKd = 8.2 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 510 10 0 5 5.3 C=CCN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL474345 179672 0 None 575 2 Rat 8.2 pKd = 8.2 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 510 10 0 5 5.3 C=CCN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44441875 169132 0 None 1513 2 Rat 8.1 pKd = 8.1 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 450 3 0 6 1.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(=O)n4C)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL440235 169132 0 None 1513 2 Rat 8.1 pKd = 8.1 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 450 3 0 6 1.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(=O)n4C)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44564783 176925 0 None -10 4 Human 8.1 pKd = 8.1 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 176925 0 None -10 4 Human 8.1 pKd = 8.1 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
44441874 154288 0 None 1548 2 Rat 8.1 pKd = 8.1 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 436 3 1 5 1.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(=O)[nH]4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL398655 154288 0 None 1548 2 Rat 8.1 pKd = 8.1 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 436 3 1 5 1.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc(=O)[nH]4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441676 94016 0 None 1258 2 Rat 8.1 pKd = 8.1 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 510 5 0 7 3.7 COc1ccc(SC)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
CHEMBL248717 94016 0 None 1258 2 Rat 8.1 pKd = 8.1 Binding
Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membraneDisplacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane
ChEMBL 510 5 0 7 3.7 COc1ccc(SC)c2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.086
44441930 94460 0 None 87 2 Rat 7.2 pKd = 7.2 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 429 2 1 3 3.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCc4c([nH]c5ccccc45)C3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL251300 94460 0 None 87 2 Rat 7.2 pKd = 7.2 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 429 2 1 3 3.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCc4c([nH]c5ccccc45)C3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL2370168 209807 0 None -1548 5 Human 5.2 pKd = 5.2 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst1) expressed in hSF6 cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst1) expressed in hSF6 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
46880588 14217 0 None 1 7 Human 6.1 pKd = 6.1 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 14217 0 None 1 7 Human 6.1 pKd = 6.1 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 14217 0 None 1 7 Human 6.1 pKd = 6.1 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
CHEMBL408752 212730 0 None -5011 4 Human 6.1 pKd = 6.1 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)
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
44564857 178938 0 None -1 4 Human 7.1 pKd = 7.1 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 178938 0 None -1 4 Human 7.1 pKd = 7.1 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
44564785 176942 0 None 112 2 Rat 7.1 pKd = 7.1 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 446 8 0 5 4.0 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCc1cccc2ccccc12 10.1016/j.bmcl.2009.01.072
CHEMBL462158 176942 0 None 112 2 Rat 7.1 pKd = 7.1 Binding
Binding affinity to rat sst1 receptorBinding affinity to rat sst1 receptor
ChEMBL 446 8 0 5 4.0 CN(CCC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1)CCc1cccc2ccccc12 10.1016/j.bmcl.2009.01.072
44441898 94224 0 None 1230 2 Rat 8.1 pKd = 8.1 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 444 3 0 5 3.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C#N)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL249932 94224 0 None 1230 2 Rat 8.1 pKd = 8.1 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 444 3 0 5 3.0 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C#N)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441877 94305 0 None 602 2 Rat 8.1 pKd = 8.1 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 494 3 0 5 4.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc5ccc(C#N)cc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250522 94305 0 None 602 2 Rat 8.1 pKd = 8.1 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 494 3 0 5 4.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc5ccc(C#N)cc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441924 94389 0 None 30 2 Rat 7.1 pKd = 7.1 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 450 3 0 3 4.7 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CC=C(c4ccc(Cl)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250912 94389 0 None 30 2 Rat 7.1 pKd = 7.1 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 450 3 0 3 4.7 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CC=C(c4ccc(Cl)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL413373 213062 0 None -269 4 Human 6.1 pKd = 6.1 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)
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
46880588 14217 0 None -1 7 Rat 6.1 pKd = 6.1 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST1 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST1 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 14217 0 None -1 7 Rat 6.1 pKd = 6.1 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST1 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST1 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 14217 0 None -1 7 Rat 6.1 pKd = 6.1 Binding
Displacement of [125I]SRIF-14 from rat cortex membrane SST1 receptorDisplacement of [125I]SRIF-14 from rat cortex membrane SST1 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
44441912 14716 0 None - 1 Rat 4.1 pKd = 4.1 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 463 4 1 5 2.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(=O)O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL1206217 14716 0 None - 1 Rat 4.1 pKd = 4.1 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 463 4 1 5 2.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(=O)O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL249894 14716 0 None - 1 Rat 4.1 pKd = 4.1 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 463 4 1 5 2.8 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc(C(=O)O)cc4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL405561 212566 0 None -316 4 Human 6.1 pKd = 6.1 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)
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
CHEMBL412466 212992 0 None -467 4 Human 6.1 pKd = 6.1 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)
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
44441876 94304 0 None 63 2 Rat 7.1 pKd = 7.1 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 469 3 0 4 4.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc5ccccc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL250521 94304 0 None 63 2 Rat 7.1 pKd = 7.1 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 469 3 0 4 4.2 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4cccc5ccccc45)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
44441887 94429 0 None 239 2 Rat 7.1 pKd = 7.1 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 460 3 0 7 2.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nccn5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
CHEMBL251121 94429 0 None 239 2 Rat 7.1 pKd = 7.1 Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membraneDisplacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL 460 3 0 7 2.1 COc1cccc2c1C[C@H]1C[C@@H](C(=O)N3CCN(c4ccc5nccn5n4)CC3)CN(C)[C@@H]1C2 10.1016/j.bmcl.2007.04.078
46880578 5545 0 None -83 2 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 5545 0 None -83 2 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
46880852 5564 0 None -107 2 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 5564 0 None -107 2 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
46880854 5566 0 None -263 2 Human 5.0 pKd = 5.0 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 5566 0 None -263 2 Human 5.0 pKd = 5.0 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
46880584 5538 0 None -758 2 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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 5538 0 None -758 2 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST1 receptorBinding affinity to human SST1 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
CHEMBL411017 212858 0 None -67 4 Human 6.0 pKd = 6.0 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst1)
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
CHEMBL3349516 211417 0 None -1 4 Human 9.8 pKi = 9.8 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
CHEMBL3349522 211422 0 None -1 4 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
CHEMBL3349521 211421 0 None -1 4 Human 9.6 pKi = 9.6 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
16129706 209031 40 None -6 5 Human 9.5 pKi = 9.5 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) 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 209031 40 None -6 5 Human 9.5 pKi = 9.5 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) 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
CHEMBL3098601 211018 0 None -1 5 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-somatostatin from human SSTR1 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR1 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
CHEMBL1823873 209032 9 None 1 4 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-somatostatin from human SSTR1 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR1 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
16129706 209031 40 None -6 5 Human 9.4 pKi = 9.4 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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 209031 40 None -6 5 Human 9.4 pKi = 9.4 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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 209031 40 None -6 5 Human 9.4 pKi = 9.4 Binding
Binding affinity towards Somatostatin receptor type 1 (hsst1)Binding affinity towards Somatostatin receptor type 1 (hsst1)
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 209031 40 None -6 5 Human 9.4 pKi = 9.4 Binding
Binding affinity towards Somatostatin receptor type 1 (hsst1)Binding affinity towards Somatostatin receptor type 1 (hsst1)
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 212710 0 None -9 5 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human sst1 receptor expressed in CHO-K1 cellsBinding affinity towards human sst1 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
16129706 209031 40 None -6 5 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-somatostatin from human SSTR1 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR1 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 209031 40 None -6 5 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-somatostatin from human SSTR1 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR1 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
CHEMBL3349517 211418 0 None -1 4 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
16129706 209031 40 None -6 5 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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 209031 40 None -6 5 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
CHEMBL3349518 211419 0 None 10 4 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
CHEMBL3349513 211414 0 None -1 4 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
CHEMBL3349605 211434 0 None -6 4 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
CHEMBL3349606 211435 0 None -15 4 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
44308969 204364 0 None 1096 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human sst1 receptor expressed in CHO-K1 cellsBinding affinity towards human sst1 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 204364 0 None 1096 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human sst1 receptor expressed in CHO-K1 cellsBinding affinity towards human sst1 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
CHEMBL442494 213913 0 None -6 5 Human 8.7 pKi = 8.7 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 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
CHEMBL3349603 211432 0 None -15 5 Human 8.0 pKi = 8 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
91809310 125785 0 None -43 4 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 1618 27 19 17 3.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3647709 125785 0 None -43 4 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 1618 27 19 17 3.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
91809283 125760 0 None -1258 6 Human 7.0 pKi = 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 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 125760 0 None -1258 6 Human 7.0 pKi = 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 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
CHEMBL2311098 209505 0 None -83 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369733 209661 0 None -5 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 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
CHEMBL2369734 209662 0 None -14 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 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
CHEMBL2369735 209663 0 None -181 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 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
CHEMBL2369750 209668 0 None -27 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cells
ChEMBL None None None CN[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC1=O 10.1021/jm0005048
CHEMBL2369751 209669 0 None -11 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cells
ChEMBL None None None CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H]1CSSC[C@H](N(C)C(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2cccnc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]([C@H](C)O)C(=O)N1 10.1021/jm0005048
CHEMBL2369752 209670 0 None -19 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 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
CHEMBL2369754 209672 0 None -107 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369755 209673 0 None -165 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369756 209674 0 None -5 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)N(C)C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369757 209675 0 None -40 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2cccnc2)CSSC[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369758 209676 0 None -36 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369759 209677 0 None 1 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)C(N)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369760 209678 0 None -42 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@@H](N)CCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369761 209679 0 None -8 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 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
CHEMBL2371893 210147 0 None -89 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 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
CHEMBL3349515 211416 0 None -12 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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 211424 0 None -10 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
142471769 191785 0 None -301 2 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 456 10 2 6 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccc(OC)cc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5198142 191785 0 None -301 2 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 456 10 2 6 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccc(OC)cc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
44387399 169017 0 None -2 3 Human 6.0 pKi = 6.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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 169017 0 None -2 3 Human 6.0 pKi = 6.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
CHEMBL385746 212364 0 None -72 4 Human 6.0 pKi = 6.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
142471841 191585 0 None -363 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1ccc2[nH]cc(Cc3nnc(Cc4ccc(F)cc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
CHEMBL5195145 191585 0 None -363 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1ccc2[nH]cc(Cc3nnc(Cc4ccc(F)cc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
91809284 125761 0 None -512 6 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 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 125761 0 None -512 6 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 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
CHEMBL385689 212359 0 None -15 4 Human 6.0 pKi = 6.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
142471716 191492 0 None -208 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5193686 191492 0 None -208 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471929 191167 0 None -676 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 414 8 2 4 4.4 Fc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5188841 191167 0 None -676 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 414 8 2 4 4.4 Fc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL414116 213111 0 None -5 4 Human 5.9 pKi = 5.9 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
90665463 109262 0 None -4 5 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst1 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 109262 0 None -4 5 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst1 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
168288485 191731 0 None -2454 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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 191731 0 None -2454 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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
CHEMBL3349514 211415 0 None -6 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
44397706 67191 0 None -70 5 Human 6.9 pKi = 6.9 Binding
Binding affinity against human sst1 receptor at a dose of 10 uMBinding affinity against human sst1 receptor at a dose of 10 uM
ChEMBL 456 9 2 6 5.4 Cc1cccc2c(CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
CHEMBL187768 67191 0 None -70 5 Human 6.9 pKi = 6.9 Binding
Binding affinity against human sst1 receptor at a dose of 10 uMBinding affinity against human sst1 receptor at a dose of 10 uM
ChEMBL 456 9 2 6 5.4 Cc1cccc2c(CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
CHEMBL2369749 209667 0 None -114 5 Human 5.9 pKi = 5.9 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 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
10296743 61838 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 receptor expressed in CHO cells
ChEMBL 436 7 3 3 5.8 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)OCc1ccccc1 10.1016/s0960-894x(01)00107-x
CHEMBL177337 61838 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 receptor expressed in CHO cells
ChEMBL 436 7 3 3 5.8 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)OCc1ccccc1 10.1016/s0960-894x(01)00107-x
CHEMBL408347 212707 0 None -117 4 Human 5.9 pKi = 5.9 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
142471978 192443 0 None -891 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 396 8 2 4 4.3 c1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5208396 192443 0 None -891 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 396 8 2 4 4.3 c1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
44385652 60392 0 None -6 5 Human 5.8 pKi = 5.8 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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 60392 0 None -6 5 Human 5.8 pKi = 5.8 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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
10210016 60435 0 None -7 3 Human 5.8 pKi = 5.8 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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 60435 0 None -7 3 Human 5.8 pKi = 5.8 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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
2054 3974 15 None -741 11 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
71306 3974 15 None -741 11 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL264186 3974 15 None -741 11 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL3349523 3974 15 None -741 11 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
DB04894 3974 15 None -741 11 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
91809287 160258 0 None -3162 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
CHEMBL4110066 160258 0 None -3162 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
90665462 109230 0 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst1 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 109230 0 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst1 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
90665460 109260 0 None -7 5 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst1 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 109260 0 None -7 5 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst1 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
CHEMBL385745 212363 0 None -15 4 Human 5.8 pKi = 5.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
142471655 190425 0 None -562 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1ccc2[nH]cc(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
CHEMBL5178013 190425 0 None -562 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1ccc2[nH]cc(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
10166743 123946 0 None -21 5 Human 5.8 pKi = 5.8 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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 123946 0 None -21 5 Human 5.8 pKi = 5.8 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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
CHEMBL275806 210823 0 None -1 4 Human 6.8 pKi = 6.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
11848679 89244 0 None -134 6 Human 5.8 pKi = 5.8 Binding
Displacement of SST14 from human recombinant SST1 receptorDisplacement of SST14 from human recombinant SST1 receptor
ChEMBL 489 9 3 9 2.9 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)cc(OCC)c1N 10.1016/j.bmcl.2009.09.024
CHEMBL236788 89244 0 None -134 6 Human 5.8 pKi = 5.8 Binding
Displacement of SST14 from human recombinant SST1 receptorDisplacement of SST14 from human recombinant SST1 receptor
ChEMBL 489 9 3 9 2.9 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)cc(OCC)c1N 10.1016/j.bmcl.2009.09.024
44397648 66764 0 None -44 5 Human 6.8 pKi = 6.8 Binding
Binding affinity against human sst1 receptor at a dose of 10 uMBinding affinity against human sst1 receptor at a dose of 10 uM
ChEMBL 476 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3c(Cl)cccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL185861 66764 0 None -44 5 Human 6.8 pKi = 6.8 Binding
Binding affinity against human sst1 receptor at a dose of 10 uMBinding affinity against human sst1 receptor at a dose of 10 uM
ChEMBL 476 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3c(Cl)cccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
44332931 4625 0 None -1047 2 Human 5.8 pKi = 5.8 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) subtype
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c(C3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/jm0108449
CHEMBL102892 4625 0 None -1047 2 Human 5.8 pKi = 5.8 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) subtype
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c(C3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/jm0108449
CHEMBL1201959 4625 0 None -1047 2 Human 5.8 pKi = 5.8 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) subtype
ChEMBL 396 3 3 2 6.1 c1ccc(-c2c[nH]c(C3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 10.1021/jm0108449
142471665 191707 0 None -602 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 414 8 2 4 4.4 Fc1ccc2c(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5196971 191707 0 None -602 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 414 8 2 4 4.4 Fc1ccc2c(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL438281 213763 0 None 1 4 Human 6.7 pKi = 6.7 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
44385757 61336 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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 61336 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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
CHEMBL3349520 211420 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
CHEMBL407496 212665 0 None -63 5 Human 5.7 pKi = 5.7 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
CHEMBL1794035 208937 0 None -7 5 Human 8.7 pKi = 8.7 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 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
16129706 209031 40 None -6 5 Human 8.6 pKi = 8.6 Binding
Binding affinity towards somatostatin receptor type 1Binding affinity towards somatostatin receptor type 1
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 209031 40 None -6 5 Human 8.6 pKi = 8.6 Binding
Binding affinity towards somatostatin receptor type 1Binding affinity towards somatostatin receptor type 1
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
10580397 99315 0 None -4 5 Human 5.7 pKi = 5.7 Binding
Binding affinity for human receptor subtype hSSTR1Binding affinity for human receptor subtype hSSTR1
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 99315 0 None -4 5 Human 5.7 pKi = 5.7 Binding
Binding affinity for human receptor subtype hSSTR1Binding affinity for human receptor subtype hSSTR1
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
142471719 190502 0 None -204 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 1 5 5.5 Cn1cc(CCc2nnc(Cc3cccc(C(F)(F)F)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
CHEMBL5179321 190502 0 None -204 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 1 5 5.5 Cn1cc(CCc2nnc(Cc3cccc(C(F)(F)F)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
13690207 115382 0 None -812 5 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst1 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 115382 0 None -812 5 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst1 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
10094509 130686 0 None -63 5 Human 5.6 pKi = 5.6 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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 130686 0 None -63 5 Human 5.6 pKi = 5.6 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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
CHEMBL429166 213509 0 None -2 4 Human 6.6 pKi = 6.6 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
15965425 2206 7 None -239883 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to human somatostatin receptor type 1Binding affinity to human somatostatin receptor type 1
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 2206 7 None -239883 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to human somatostatin receptor type 1Binding affinity to human somatostatin receptor type 1
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 2206 7 None -239883 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to human somatostatin receptor type 1Binding affinity to human somatostatin receptor type 1
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 2206 7 None -239883 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards Somatostatin receptor type 1 (hsst1)Binding affinity towards Somatostatin receptor type 1 (hsst1)
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 2206 7 None -239883 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards Somatostatin receptor type 1 (hsst1)Binding affinity towards Somatostatin receptor type 1 (hsst1)
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 2206 7 None -239883 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards Somatostatin receptor type 1 (hsst1)Binding affinity towards Somatostatin receptor type 1 (hsst1)
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
91809303 125778 0 None -75 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 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 125778 0 None -75 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 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
10325243 100495 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity for human receptor subtype hSSTR1Binding affinity for human receptor subtype hSSTR1
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 100495 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity for human receptor subtype hSSTR1Binding affinity for human receptor subtype hSSTR1
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
44309052 203947 0 None -123 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human sst1 receptor expressed in CHO-K1 cellsBinding affinity towards human sst1 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 203947 0 None -123 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human sst1 receptor expressed in CHO-K1 cellsBinding affinity towards human sst1 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
13690207 115382 0 None -812 5 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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 115382 0 None -812 5 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
44385504 61048 0 None -6 5 Human 5.6 pKi = 5.6 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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 61048 0 None -6 5 Human 5.6 pKi = 5.6 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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
142471684 191452 0 None -1174 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5193172 191452 0 None -1174 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
91809306 125781 0 None -190 4 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 1738 28 16 17 6.7 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](N(CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647705 125781 0 None -190 4 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 1738 28 16 17 6.7 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](N(CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
10411795 130619 0 None -15 3 Human 5.6 pKi = 5.6 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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 130619 0 None -15 3 Human 5.6 pKi = 5.6 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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
142471848 191267 0 None -263 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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 191267 0 None -263 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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
44385712 60344 0 None -4 4 Human 5.6 pKi = 5.6 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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 60344 0 None -4 4 Human 5.6 pKi = 5.6 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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
91809320 126378 0 None -50 3 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 1897 34 19 18 6.5 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](CCCCNC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL3650456 126378 0 None -50 3 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 1897 34 19 18 6.5 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](CCCCNC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
44377555 57531 0 None -4 5 Human 5.5 pKi = 5.5 Binding
Inhibitory constant on human Somatostatin receptor type 1Inhibitory constant on human Somatostatin receptor type 1
ChEMBL 384 5 1 5 5.2 NCCCc1nc(-c2csc3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
CHEMBL166247 57531 0 None -4 5 Human 5.5 pKi = 5.5 Binding
Inhibitory constant on human Somatostatin receptor type 1Inhibitory constant on human Somatostatin receptor type 1
ChEMBL 384 5 1 5 5.2 NCCCc1nc(-c2csc3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
CHEMBL3349601 211430 0 None -5 4 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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 211431 0 None -10 5 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
10009650 99795 0 None -3 4 Human 6.5 pKi = 6.5 Binding
Binding affinity for human receptor subtype hSSTR1Binding affinity for human receptor subtype hSSTR1
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 99795 0 None -3 4 Human 6.5 pKi = 6.5 Binding
Binding affinity for human receptor subtype hSSTR1Binding affinity for human receptor subtype hSSTR1
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
13690207 115382 0 None -812 5 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-somatostatin from human SSTR1 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR1 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 115382 0 None -812 5 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-somatostatin from human SSTR1 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR1 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
142471737 190304 0 None -77 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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 190304 0 None -77 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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
91809277 125754 0 None -107 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 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 125754 0 None -107 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 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
71461645 78904 0 None -4 4 Human 5.5 pKi = 5.5 Binding
Inhibitory constant on human Somatostatin receptor type 1Inhibitory constant on human Somatostatin receptor type 1
ChEMBL 367 5 2 4 4.4 NCCCc1nc(-c2c[nH]c3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
CHEMBL2112935 78904 0 None -4 4 Human 5.5 pKi = 5.5 Binding
Inhibitory constant on human Somatostatin receptor type 1Inhibitory constant on human Somatostatin receptor type 1
ChEMBL 367 5 2 4 4.4 NCCCc1nc(-c2c[nH]c3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
CHEMBL438726 213789 0 None 2 4 Human 7.5 pKi = 7.5 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
10248767 57192 0 None -7 4 Human 5.5 pKi = 5.5 Binding
Inhibitory constant on human Somatostatin receptor type 1Inhibitory constant on human Somatostatin receptor type 1
ChEMBL 373 6 1 6 3.9 NCCCc1nc(-c2cccc([N+](=O)[O-])c2)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
CHEMBL164964 57192 0 None -7 4 Human 5.5 pKi = 5.5 Binding
Inhibitory constant on human Somatostatin receptor type 1Inhibitory constant on human Somatostatin receptor type 1
ChEMBL 373 6 1 6 3.9 NCCCc1nc(-c2cccc([N+](=O)[O-])c2)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
44386389 130083 0 None -6 5 Human 5.5 pKi = 5.5 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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 130083 0 None -6 5 Human 5.5 pKi = 5.5 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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
CHEMBL414386 213129 0 None -4 4 Human 6.5 pKi = 6.5 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
142471801 192299 0 None -199 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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 192299 0 None -199 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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
142471923 191911 0 None -512 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 488 10 2 6 3.9 CS(=O)(=O)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5200112 191911 0 None -512 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 488 10 2 6 3.9 CS(=O)(=O)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL406491 212611 0 None 4 4 Human 7.4 pKi = 7.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
2070 697 5 None -5888 4 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-1) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/jm0108449
9802572 697 5 None -5888 4 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-1) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/jm0108449
CHEMBL2069499 697 5 None -5888 4 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-1) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/jm0108449
CHEMBL437448 213719 0 None -23 5 Human 6.4 pKi = 6.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
91809275 125752 0 None -316 6 Human 7.4 pKi = 7.4 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 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 125752 0 None -316 6 Human 7.4 pKi = 7.4 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 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
CHEMBL2369753 209671 0 None -4 5 Human 6.4 pKi = 6.4 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 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
9852911 99383 0 None -26 6 Human 5.4 pKi = 5.4 Binding
Binding affinity for human receptor subtype hSSTR1Binding affinity for human receptor subtype hSSTR1
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 99383 0 None -26 6 Human 5.4 pKi = 5.4 Binding
Binding affinity for human receptor subtype hSSTR1Binding affinity for human receptor subtype hSSTR1
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
10770814 100792 0 None -2 5 Human 5.4 pKi = 5.4 Binding
Binding affinity for human receptor subtype hSSTR1Binding affinity for human receptor subtype hSSTR1
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 100792 0 None -2 5 Human 5.4 pKi = 5.4 Binding
Binding affinity for human receptor subtype hSSTR1Binding affinity for human receptor subtype hSSTR1
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
44377591 55633 0 None -1 4 Human 5.4 pKi = 5.4 Binding
Inhibitory constant on human Somatostatin receptor type 1Inhibitory constant on human Somatostatin receptor type 1
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 55633 0 None -1 4 Human 5.4 pKi = 5.4 Binding
Inhibitory constant on human Somatostatin receptor type 1Inhibitory constant on human Somatostatin receptor type 1
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
142471961 191421 0 None -275 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 494 10 2 5 5.4 FC(F)(F)Oc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5192791 191421 0 None -275 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 494 10 2 5 5.4 FC(F)(F)Oc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
91809285 125762 0 None -323 6 Human 7.4 pKi = 7.4 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 125762 0 None -323 6 Human 7.4 pKi = 7.4 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
91809301 125776 0 None -831 4 Human 7.4 pKi = 7.4 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 1470 22 17 16 2.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3647700 125776 0 None -831 4 Human 7.4 pKi = 7.4 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 1470 22 17 16 2.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
9985523 99161 0 None -2 5 Human 5.4 pKi = 5.4 Binding
Binding affinity for human receptor subtype hSSTR1Binding affinity for human receptor subtype hSSTR1
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 99161 0 None -2 5 Human 5.4 pKi = 5.4 Binding
Binding affinity for human receptor subtype hSSTR1Binding affinity for human receptor subtype hSSTR1
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
CHEMBL408987 212740 0 None -2 5 Human 6.4 pKi = 6.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
CHEMBL410181 212805 0 None -1 5 Human 6.4 pKi = 6.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
9848232 102153 0 None -6 3 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human sst1 receptor expressed in CHO-K1 cellsBinding affinity towards human sst1 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 102153 0 None -6 3 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human sst1 receptor expressed in CHO-K1 cellsBinding affinity towards human sst1 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
142471733 190565 0 None -75 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 394 7 2 4 4.4 CC(C)(C)Cc1nnc(Cc2c[nH]c3cc(F)ccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5180116 190565 0 None -75 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 394 7 2 4 4.4 CC(C)(C)Cc1nnc(Cc2c[nH]c3cc(F)ccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL407195 212646 0 None -21 4 Human 6.4 pKi = 6.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
10699714 99417 0 None -2 5 Human 5.4 pKi = 5.4 Binding
Binding affinity for human receptor subtype hSSTR1Binding affinity for human receptor subtype hSSTR1
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 99417 0 None -2 5 Human 5.4 pKi = 5.4 Binding
Binding affinity for human receptor subtype hSSTR1Binding affinity for human receptor subtype hSSTR1
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
73348312 89238 0 None -4897 2 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-1) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) 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 89238 0 None -4897 2 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-1) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) subtype
ChEMBL 410 3 3 2 6.2 CC1(C2CCCCC2)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL439005 213817 0 None -8 4 Human 6.4 pKi = 6.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
168274800 190092 0 None -630 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 2 6 3.8 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5172814 190092 0 None -630 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 2 6 3.8 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
16062816 6064 0 None -1479 5 Human 5.4 pKi = 5.4 Binding
Displacement of SST14 from human recombinant SST1 receptorDisplacement of SST14 from human recombinant SST1 receptor
ChEMBL 473 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(C(=O)O)ccc4o3)CC2)cc(OCC)c1Cl 10.1016/j.bmcl.2009.09.024
CHEMBL1080585 6064 0 None -1479 5 Human 5.4 pKi = 5.4 Binding
Displacement of SST14 from human recombinant SST1 receptorDisplacement of SST14 from human recombinant SST1 receptor
ChEMBL 473 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(C(=O)O)ccc4o3)CC2)cc(OCC)c1Cl 10.1016/j.bmcl.2009.09.024
86294248 118820 1 None -1023 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 1 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 1 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 298 3 2 4 1.4 Cn1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc21 10.1021/ml500538a
CHEMBL3421843 118820 1 None -1023 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 1 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 1 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 298 3 2 4 1.4 Cn1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc21 10.1021/ml500538a
71458043 78903 0 None -3 5 Human 5.3 pKi = 5.3 Binding
Inhibitory constant on human Somatostatin receptor type 1Inhibitory constant on human Somatostatin receptor type 1
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 78903 0 None -3 5 Human 5.3 pKi = 5.3 Binding
Inhibitory constant on human Somatostatin receptor type 1Inhibitory constant on human Somatostatin receptor type 1
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
142471924 190394 0 None -524 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 432 8 2 4 4.6 Fc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5177573 190394 0 None -524 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 432 8 2 4 4.6 Fc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
91809300 125775 0 None -602 4 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1454 22 16 15 2.7 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647699 125775 0 None -602 4 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1454 22 16 15 2.7 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
142471772 191178 0 None -870 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 488 9 2 4 5.3 Brc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5189042 191178 0 None -870 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 488 9 2 4 5.3 Brc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
56945132 171420 0 None -251 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF from SST1 receptor (unknown origin) after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from SST1 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 171420 0 None -251 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF from SST1 receptor (unknown origin) after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from SST1 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
CHEMBL415201 213180 0 None -13 4 Human 6.3 pKi = 6.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
46882133 5808 0 None -27 7 Human 5.3 pKi = 5.3 Binding
Displacement of SST14 from human recombinant SST1 receptorDisplacement of SST14 from human recombinant SST1 receptor
ChEMBL 478 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NC(=O)C5CCC5)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1078896 5808 0 None -27 7 Human 5.3 pKi = 5.3 Binding
Displacement of SST14 from human recombinant SST1 receptorDisplacement of SST14 from human recombinant SST1 receptor
ChEMBL 478 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NC(=O)C5CCC5)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
91809308 125783 0 None -15 4 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1602 27 18 16 4.2 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647707 125783 0 None -15 4 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1602 27 18 16 4.2 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
9857566 60060 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 receptor expressed in CHO cells
ChEMBL 302 4 3 2 3.8 N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1 10.1016/s0960-894x(01)00107-x
CHEMBL173715 60060 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 receptor expressed in CHO cells
ChEMBL 302 4 3 2 3.8 N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1 10.1016/s0960-894x(01)00107-x
CHEMBL1201185 208601 28 None -1000 4 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
11963995 91865 0 None -295 3 Human 5.3 pKi = 5.3 Binding
Binding affinity to human SST1RBinding affinity to human SST1R
ChEMBL 387 6 1 4 3.8 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)ccc1Cl 10.1021/jm701144e
CHEMBL241329 91865 0 None -295 3 Human 5.3 pKi = 5.3 Binding
Binding affinity to human SST1RBinding affinity to human SST1R
ChEMBL 387 6 1 4 3.8 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)ccc1Cl 10.1021/jm701144e
CHEMBL413171 213051 0 None -4 5 Human 6.3 pKi = 6.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
11705763 168315 0 None -1380 5 Human 6.3 pKi = 6.3 Binding
Binding affinity against human sst1 receptor at a dose of 10 uMBinding affinity against human sst1 receptor at a dose of 10 uM
ChEMBL 484 10 2 7 5.4 Cc1cccc2c(C(=O)CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
CHEMBL434159 168315 0 None -1380 5 Human 6.3 pKi = 6.3 Binding
Binding affinity against human sst1 receptor at a dose of 10 uMBinding affinity against human sst1 receptor at a dose of 10 uM
ChEMBL 484 10 2 7 5.4 Cc1cccc2c(C(=O)CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
142471677 191949 0 None -1621 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 478 9 2 4 5.5 FC(F)(F)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5200786 191949 0 None -1621 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 478 9 2 4 5.5 FC(F)(F)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
44308836 102791 0 None -134 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human sst1 receptor expressed in CHO-K1 cellsBinding affinity towards human sst1 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 102791 0 None -134 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human sst1 receptor expressed in CHO-K1 cellsBinding affinity towards human sst1 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
9827283 78588 0 None -117 4 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human sst1 receptor expressed in CHO-K1 cellsBinding affinity towards human sst1 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 78588 0 None -117 4 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human sst1 receptor expressed in CHO-K1 cellsBinding affinity towards human sst1 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
142471936 191495 0 None -776 5 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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 191495 0 None -776 5 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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
CHEMBL437057 213703 0 None -3 3 Human 6.3 pKi = 6.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
CHEMBL264028 210603 0 None -32 5 Human 6.2 pKi = 6.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
44397389 124044 0 None -33 5 Human 7.2 pKi = 7.2 Binding
Binding affinity against human sst1 receptor at a dose of 10 uMBinding affinity against human sst1 receptor at a dose of 10 uM
ChEMBL 460 9 2 6 5.2 NCCCCn1c(SCCc2c[nH]c3cc(F)ccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL363092 124044 0 None -33 5 Human 7.2 pKi = 7.2 Binding
Binding affinity against human sst1 receptor at a dose of 10 uMBinding affinity against human sst1 receptor at a dose of 10 uM
ChEMBL 460 9 2 6 5.2 NCCCCn1c(SCCc2c[nH]c3cc(F)ccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
142471730 190385 0 None -741 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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 190385 0 None -741 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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
91809302 125777 0 None -26 3 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1439 23 16 14 3.7 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647701 125777 0 None -26 3 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1439 23 16 14 3.7 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
91809291 125766 0 None -120 4 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1473 23 16 14 2.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCC[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL3647690 125766 0 None -120 4 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1473 23 16 14 2.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCC[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
2018 3007 28 None -50 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
9941444 3007 28 None -50 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL3349607 3007 28 None -50 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
DB06663 3007 28 None -50 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL3349524 211423 0 None -10 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
CHEMBL3349604 211433 0 None -15 5 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
91809286 125763 0 None -41 6 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 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 125763 0 None -41 6 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 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
CHEMBL411556 212886 0 None 1 4 Human 7.2 pKi = 7.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
142471891 190595 0 None -436 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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 190595 0 None -436 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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
CHEMBL3349599 211428 0 None -199 5 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
CHEMBL421362 213274 0 None -1258 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 1 (sst1) 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
91809292 125767 0 None -3235 4 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1619 27 18 17 2.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647691 125767 0 None -3235 4 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1619 27 18 17 2.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
90644981 111813 0 None -173 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]SS14 from human SST1 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST1 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 111813 0 None -173 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]SS14 from human SST1 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST1 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
142471678 190042 0 None -660 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 474 9 2 6 3.7 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5171935 190042 0 None -660 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 474 9 2 6 3.7 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
10554930 100192 0 None -2 5 Human 5.2 pKi = 5.2 Binding
Binding affinity for human receptor subtype hSSTR1Binding affinity for human receptor subtype hSSTR1
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 100192 0 None -2 5 Human 5.2 pKi = 5.2 Binding
Binding affinity for human receptor subtype hSSTR1Binding affinity for human receptor subtype hSSTR1
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
91809296 125771 0 None -34673 4 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1488 23 17 17 1.5 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCS(=O)(=O)C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3647695 125771 0 None -34673 4 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1488 23 17 17 1.5 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCS(=O)(=O)C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL414598 213146 0 None 1 4 Human 7.2 pKi = 7.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
142471767 192282 0 None -1348 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 4 5.1 Clc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5205904 192282 0 None -1348 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 4 5.1 Clc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
44363816 39675 0 None -194 5 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 1 (hSSTR-1)In vitro binding affinity was evaluated against human Somatostatin receptor type 1 (hSSTR-1)
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 39675 0 None -194 5 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 1 (hSSTR-1)In vitro binding affinity was evaluated against human Somatostatin receptor type 1 (hSSTR-1)
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
CHEMBL2372959 210325 0 None -2 5 Human 6.1 pKi = 6.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
117711399 118822 0 None -104 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 1 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 1 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 310 3 2 4 1.8 Cc1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc2n1 10.1021/ml500538a
CHEMBL3421845 118822 0 None -104 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 1 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 1 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 310 3 2 4 1.8 Cc1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc2n1 10.1021/ml500538a
91809290 125765 0 None -213 4 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 1636 27 18 16 3.3 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL3647689 125765 0 None -213 4 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 1636 27 18 16 3.3 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL406152 212596 0 None 1 4 Human 7.1 pKi = 7.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
90665461 109261 0 None -4 5 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst1 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 109261 0 None -4 5 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst1 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
CHEMBL406738 212618 0 None -11 5 Human 6.1 pKi = 6.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 1The compound was tested for binding affinity against human Somatostatin receptor type 1
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
86293506 118819 0 None -229 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 1 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 1 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 309 3 2 3 2.4 Cc1cc2ccccc2c(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)n1 10.1021/ml500538a
CHEMBL3421842 118819 0 None -229 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 1 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 1 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 309 3 2 3 2.4 Cc1cc2ccccc2c(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)n1 10.1021/ml500538a
168275406 190307 0 None -794 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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 190307 0 None -794 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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
13690207 115382 0 None -812 5 Human 6.1 pKi = 6.1 Binding
Binding affinity towards somatostatin receptor type 1Binding affinity towards somatostatin receptor type 1
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 115382 0 None -812 5 Human 6.1 pKi = 6.1 Binding
Binding affinity towards somatostatin receptor type 1Binding affinity towards somatostatin receptor type 1
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
91809276 125753 0 None -26 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 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 125753 0 None -26 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 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
91809294 125769 0 None -1148 4 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1912 34 19 19 3.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](CCCCNC(=O)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647693 125769 0 None -1148 4 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1912 34 19 19 3.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](CCCCNC(=O)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
44385591 131387 0 None -38 2 Human 5.0 pKi = 5.0 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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 131387 0 None -38 2 Human 5.0 pKi = 5.0 Binding
Inhibition of human sst1 receptor expressed in CHO cellsInhibition of human sst1 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
142471832 190275 0 None -138 5 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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 190275 0 None -138 5 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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
10096510 57428 0 None -26 4 Human 5.0 pKi = 5.0 Binding
Inhibitory constant on human Somatostatin receptor type 1Inhibitory constant on human Somatostatin receptor type 1
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 57428 0 None -26 4 Human 5.0 pKi = 5.0 Binding
Inhibitory constant on human Somatostatin receptor type 1Inhibitory constant on human Somatostatin receptor type 1
ChEMBL 475 7 2 6 5.2 CC(C)(C(=O)NC1CCCCC1)c1cn2cc(-c3csc4ccccc34)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
168279197 190932 0 None -1621 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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 190932 0 None -1621 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST1 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST1 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
91809288 125764 0 None -562 6 Human 7.0 pKi = 7 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1472 23 17 16 1.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCC[S@@+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3647688 125764 0 None -562 6 Human 7.0 pKi = 7 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1472 23 17 16 1.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCC[S@@+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
91809312 125787 0 None -588 3 Human 7.0 pKi = 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 1754 28 17 18 6.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](N(CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3647711 125787 0 None -588 3 Human 7.0 pKi = 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 1754 28 17 18 6.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](N(CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
2030 3672 10 None -13 10 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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-] 15135911
5311377 3672 10 None -13 10 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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-] 15135911
CHEMBL251541 3672 10 None -13 10 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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-] 15135911
16161315 216096 0 125I-CGP23996 -6 12 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 216096 0 125I-Tyr11-SRIF -6 12 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 216096 0 UNDEFINED -6 12 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 216096 0 125I-Tyr11-somatostatin -3 12 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 216096 0 125I-Tyr11-somatostatin-14 -3 12 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-Tyr11-SRIF-14 -6 12 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 216096 0 125I-LTT-SST-28 -6 12 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-LTT-SST-28 -6 12 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-Tyr11-SRIF -6 12 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-SOMATOSTATIN 14 -6 12 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 216096 0 125I-SRIF -6 12 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 216096 0 125I-SRIF-28 -6 12 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 216096 0 125I-LTT-SRIF28 -6 12 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 216096 0 125I-LTT-SRIF28 -6 12 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 216096 0 125I-Tyr11-SRIF -6 12 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 216096 0 125I-Tyr10-CST14 -6 12 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 216096 0 125I-Tyr11-somatostatin-14 -6 12 Human 9.0 pKi = 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 216096 0 125I-LTT-SST-28 -6 12 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-CGP23996 -6 12 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
2055 2907 48 125I-CGP23996 -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-LTT-SST-28 -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-Tyr11-SRIF -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-Tyr11-somatostatin-14 -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-CGP23996 -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-LTT-SST-28 -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-Tyr11-SRIF -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-Tyr11-somatostatin-14 -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-CGP23996 -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-LTT-SST-28 -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-Tyr11-SRIF -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-Tyr11-somatostatin-14 -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-CGP23996 -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-LTT-SST-28 -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-Tyr11-SRIF -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-Tyr11-somatostatin-14 -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-CGP23996 -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-LTT-SST-28 -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-Tyr11-SRIF -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-Tyr11-somatostatin-14 -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-CGP23996 -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-LTT-SST-28 -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-Tyr11-SRIF -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-Tyr11-somatostatin-14 -1047 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3974 15 125I-LTT-SST-28 -741 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3974 15 UNDEFINED -741 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-LTT-SST-28 -741 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 UNDEFINED -741 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-LTT-SST-28 -741 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 UNDEFINED -741 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-LTT-SST-28 -741 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 UNDEFINED -741 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-LTT-SST-28 -741 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 UNDEFINED -741 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216097 0 125I-CGP23996 -19054 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 216097 0 125I-LTT-SST-28 -19054 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 216097 0 125I-SOMATOSTATIN -19054 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 216097 0 125I-SRIF -19054 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 216097 0 125I-SRIF-28 -19054 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 216097 0 125I-Tyr11-SRIF -19054 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 216097 0 125I-Tyr11-somatostatin-14 -19054 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
13105142 216098 0 UNDEFINED -30199 5 Human 6.0 pKi = 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
None 216097 0 125I-LTT-SST-28 -19054 11 Human 5.0 pKi = 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 216097 0 125I-Tyr11-SRIF -19054 11 Human 5.0 pKi = 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
13105142 216098 0 125I-CGP23996 -30199 5 Human 5.0 pKi = 5 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 216098 0 125I-LTT-SRIF28 -30199 5 Human 5.0 pKi = 5 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 216098 0 125I-Tyr10-CST14 -30199 5 Human 5.0 pKi = 5 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 216348 0 125I-LTT-SST-28 -93 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 584 17 5 8 2.8 CCCCC(C(=O)NC(CCCCN)C(=O)OC)NC(=O)NC(CC1=CC=CC=C1)C(=O)NC2=CC=C(C=C2)[N+](=O)[O-] None
2054 3974 15 125I-Tyr10-CST14 -741 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-Tyr10-CST14 -741 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-Tyr10-CST14 -741 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-Tyr10-CST14 -741 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-Tyr10-CST14 -741 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3974 15 125I-Tyr10-CST14 -741 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-Tyr10-CST14 -741 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-Tyr10-CST14 -741 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-Tyr10-CST14 -741 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-Tyr10-CST14 -741 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-Tyr11-somatostatin-14 -1047 14 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-Tyr11-somatostatin-14 -1047 14 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-Tyr11-somatostatin-14 -1047 14 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-Tyr11-somatostatin-14 -1047 14 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-Tyr11-somatostatin-14 -1047 14 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-Tyr11-somatostatin-14 -1047 14 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-Tyr11-SRIF -1047 14 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-Tyr11-SRIF -1047 14 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-Tyr11-SRIF -1047 14 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-Tyr11-SRIF -1047 14 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-Tyr11-SRIF -1047 14 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-Tyr11-SRIF -1047 14 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216348 0 125I-LTT-SST-28 -93 5 Human 5.9 pKi = 5.9 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 216348 0 UNDEFINED -93 5 Human 5.9 pKi = 5.9 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
2054 3974 15 125I-SRIF-28 -741 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3974 15 125I-Tyr11-SRIF -741 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-SRIF-28 -741 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-Tyr11-SRIF -741 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-SRIF-28 -741 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-Tyr11-SRIF -741 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-SRIF-28 -741 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-Tyr11-SRIF -741 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-SRIF-28 -741 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-Tyr11-SRIF -741 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3974 15 125I-SRIF -741 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-SRIF -741 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-SRIF -741 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-SRIF -741 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-SRIF -741 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216346 0 125I-Tyr11-somatostatin-14 -112 8 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 1077 14 12 13 0.6 CC(C1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=CC=C4)CC5=CC=CC=C5)N)C(=O)N)CC6=CC=CC=C6)O None
None 216346 0 UNDEFINED -112 8 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 1077 14 12 13 0.6 CC(C1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=CC=C4)CC5=CC=CC=C5)N)C(=O)N)CC6=CC=CC=C6)O None
None 216349 0 125I-LTT-SST-28 -537 5 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 485 11 4 4 3.1 COC(=O)C(CCCN=C(N)N)NC(=O)CCCC1=C(NC2=C(C=C(C=C12)F)F)C3=CC=CC=C3 None
None 216349 0 UNDEFINED -537 5 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 485 11 4 4 3.1 COC(=O)C(CCCN=C(N)N)NC(=O)CCCC1=C(NC2=C(C=C(C=C12)F)F)C3=CC=CC=C3 None
16161315 216096 0 125I-Tyr11-SRIF -6 12 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
16161315 216096 0 125I-Tyr11-somatostatin-14 -6 12 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
16161315 216096 0 125I-SOMATOSTATIN -6 12 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
16161315 216096 0 125I-Tyr11-somatostatin-14 -6 12 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 2907 48 125I-LTT-SRIF28 -1047 14 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-LTT-SRIF28 -1047 14 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-LTT-SRIF28 -1047 14 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-LTT-SRIF28 -1047 14 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-LTT-SRIF28 -1047 14 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-LTT-SRIF28 -1047 14 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3974 15 125I-CGP23996 -741 11 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-CGP23996 -741 11 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-CGP23996 -741 11 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-CGP23996 -741 11 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-CGP23996 -741 11 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-LTT-SST-28 -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-LTT-SST-28 -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-LTT-SST-28 -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-LTT-SST-28 -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-LTT-SST-28 -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-LTT-SST-28 -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-SRIF-28 -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-SRIF-28 -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-SRIF-28 -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-SRIF-28 -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-SRIF-28 -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-SRIF-28 -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-SOMATOSTATIN 14 -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-SRIF -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-SOMATOSTATIN 14 -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-SRIF -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-SOMATOSTATIN 14 -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-SRIF -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-SOMATOSTATIN 14 -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-SRIF -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-SOMATOSTATIN 14 -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-SRIF -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-SOMATOSTATIN 14 -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-SRIF -1047 14 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216347 0 125I-LTT-SST-28 -54954 5 Human 5.6 pKi = 5.6 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 216347 0 UNDEFINED -54954 5 Human 5.6 pKi = 5.6 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
2055 2907 48 UNDEFINED -1047 14 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 UNDEFINED -1047 14 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 UNDEFINED -1047 14 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 UNDEFINED -1047 14 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 UNDEFINED -1047 14 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 UNDEFINED -1047 14 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216350 0 125I-LTT-SST-28 -4 5 Human 8.5 pKi = 8.5 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 216350 0 UNDEFINED -4 5 Human 8.5 pKi = 8.5 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 2907 48 125I-Tyr10-CST14 -1047 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-Tyr10-CST14 -1047 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-Tyr10-CST14 -1047 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-Tyr10-CST14 -1047 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-Tyr10-CST14 -1047 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-Tyr10-CST14 -1047 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-Tyr10-CST14 -1047 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-Tyr10-CST14 -1047 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-Tyr10-CST14 -1047 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-Tyr10-CST14 -1047 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-Tyr10-CST14 -1047 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-Tyr10-CST14 -1047 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 216096 0 125I-Tyr11-SRIF -3 12 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 3974 15 125I-SOMATOSTATIN -741 11 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-SOMATOSTATIN -741 11 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-SOMATOSTATIN -741 11 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-SOMATOSTATIN -741 11 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-SOMATOSTATIN -741 11 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2031 2273 0 UNDEFINED -851 9 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase None None None None None
71349 2273 0 UNDEFINED -851 9 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB06791 2273 0 UNDEFINED -851 9 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216495 0 125I-LTT-SST-28 -11220 5 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216346 0 125I-SOMATOSTATIN -112 8 Human 6.2 pKi = 6.2 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
2055 2907 48 125I-CGP23996 -1047 14 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-CGP23996 -1047 14 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-CGP23996 -1047 14 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-CGP23996 -1047 14 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-CGP23996 -1047 14 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-CGP23996 -1047 14 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 None -1047 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
383414 2907 48 None -1047 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
90488715 2907 48 None -1047 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
CHEMBL1680 2907 48 None -1047 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
CHEMBL262746 2907 48 None -1047 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
DB00104 2907 48 None -1047 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
2054 3974 15 125I-LTT-SRIF28 -741 11 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-LTT-SRIF28 -741 11 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-LTT-SRIF28 -741 11 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-LTT-SRIF28 -741 11 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-LTT-SRIF28 -741 11 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3974 15 125I-LTT-SRIF28 -741 11 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-LTT-SRIF28 -741 11 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-LTT-SRIF28 -741 11 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-LTT-SRIF28 -741 11 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-LTT-SRIF28 -741 11 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-SOMATOSTATIN -1047 14 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-SOMATOSTATIN -1047 14 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-SOMATOSTATIN -1047 14 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-SOMATOSTATIN -1047 14 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-SOMATOSTATIN -1047 14 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-SOMATOSTATIN -1047 14 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 216096 0 None -6 12 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-1) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) 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
2028 1506 0 None -2238 6 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12616335
2029 2375 0 None -281 6 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12616335
2014 2214 0 None -281 9 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2014 2214 0 None -281 9 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2017 2744 0 None -10 3 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
16130961 891 0 None -5 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
16130961 891 0 None -5 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
16130961 891 0 None -5 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2005 891 0 None -5 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2005 891 0 None -5 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2005 891 0 None -5 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2007 1170 0 None -12 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2007 1170 0 None -12 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2015 2257 0 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 607 16 3 4 6.2 NCCC(CC(CNC(=O)[C@@H](Cc1cccc2c1cccc2)NC(=O)N(CCc1ccccn1)CCc1ccccc1)(C)C)C 9784130
9938757 2257 0 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 607 16 3 4 6.2 NCCC(CC(CNC(=O)[C@@H](Cc1cccc2c1cccc2)NC(=O)N(CCc1ccccn1)CCc1ccccc1)(C)C)C 9784130
154734381 217714 0 None 1 8 Human 8.2 pKi None 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
2004 642 0 None -4 7 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2004 642 0 None -4 7 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2004 642 0 None -4 7 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2016 2260 4 None -7 2 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 536 11 4 5 5.2 NCCCC[C@@H](C(=O)OC[C@@H](N)C)NC(=O)Cc1c([nH]c2c1ccc1c2cccc1)c1ccc2c(c1)cccc2 9784130
5311375 2260 4 None -7 2 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 536 11 4 5 5.2 NCCCC[C@@H](C(=O)OC[C@@H](N)C)NC(=O)Cc1c([nH]c2c1ccc1c2cccc1)c1ccc2c(c1)cccc2 9784130
CHEMBL252764 2260 4 None -7 2 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 536 11 4 5 5.2 NCCCC[C@@H](C(=O)OC[C@@H](N)C)NC(=O)Cc1c([nH]c2c1ccc1c2cccc1)c1ccc2c(c1)cccc2 9784130
16133849 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
16133849 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
16133849 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
16133849 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
16133849 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
16133849 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2020 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2020 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
2020 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2020 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2020 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2020 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
91935900 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
91935900 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
91935900 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
91935900 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
91935900 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
91935900 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL501796 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL501796 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
CHEMBL501796 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL501796 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL501796 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL501796 3676 12 None -7 9 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2019 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2019 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11520208
2019 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
2019 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2019 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2019 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2019 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2019 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
2019 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
44386062 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
44386062 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11520208
44386062 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
44386062 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
44386062 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
44386062 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
44386062 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
44386062 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
44386062 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
CHEMBL440072 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL440072 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11520208
CHEMBL440072 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
CHEMBL440072 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL440072 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL440072 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL440072 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL440072 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
CHEMBL440072 3675 0 None -4 10 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
2008 1211 0 None 1 6 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2008 1211 0 None 1 6 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
2008 1211 0 None 1 6 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799