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Assay Detail

CHEMBL972316

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human cloned sst1 receptor
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Somatostatin receptor type 1 (CHEMBL1917)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Ring size of somatostatin analogues (ODT-8) modulates receptor selectivity and binding affinity.
Erchegyi J, Grace CR, Samant M, Cescato R, Piccand V, Riek R, Reubi JC, Rivier JE.
J Med Chem (2008) 51 : 2668 -2675
PubMed 18410084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.15 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL442494 1 8.49
CHEMBL500326 1 7.85
CHEMBL446380 1 7.80
CHEMBL504457 1 7.66
CHEMBL452157 1 7.57
CHEMBL505128 1 7.10
CHEMBL504087 1 7.02
CHEMBL504248 1 6.66
CHEMBL447989 1 6.52
CHEMBL504395 1 6.45
CHEMBL525030 1 6.38
CHEMBL503036 1 6.27
CHEMBL504462 1 -
CHEMBL453936 1 -
CHEMBL525397 1 -
CHEMBL502511 1 -
CHEMBL505854 1 -
CHEMBL503596 1 -
CHEMBL524870 1 -
CHEMBL505496 1 -
CHEMBL501776 1 -
CHEMBL502777 1 -
CHEMBL506892 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL442494 IC50 = 3.2 nM 8.49
CHEMBL500326 IC50 = 14.0 nM 7.85
CHEMBL446380 IC50 = 16.0 nM 7.80
CHEMBL504457 IC50 = 22.0 nM 7.66
CHEMBL452157 IC50 = 27.0 nM 7.57
CHEMBL505128 IC50 = 79.0 nM 7.10
CHEMBL504087 IC50 = 96.0 nM 7.02
CHEMBL504248 IC50 = 218.0 nM 6.66
CHEMBL447989 IC50 = 302.0 nM 6.52
CHEMBL504395 IC50 = 358.0 nM 6.45
CHEMBL525030 IC50 = 416.0 nM 6.38
CHEMBL503036 IC50 = 540.0 nM 6.27
CHEMBL504462 IC50 > 1000.0 nM -
CHEMBL453936 IC50 > 1000.0 nM -
CHEMBL525397 IC50 > 1000.0 nM -
CHEMBL502511 IC50 > 1000.0 nM -
CHEMBL505854 IC50 > 1000.0 nM -
CHEMBL503596 IC50 > 1000.0 nM -
CHEMBL524870 IC50 > 1000.0 nM -
CHEMBL505496 IC50 > 1000.0 nM -
CHEMBL501776 IC50 > 1000.0 nM -
CHEMBL502777 IC50 > 1000.0 nM -
CHEMBL506892 IC50 > 1000.0 nM -