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Assay Detail

CHEMBL805041

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

Binding
Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Novel sst(4)-selective somatostatin (SRIF) agonists. 3. Analogues amenable to radiolabeling.
Erchegyi J, Waser B, Schaer JC, Cescato R, Brazeau JF, Rivier J, Reubi JC.
J Med Chem (2003) 46 : 5597 -5605
PubMed 14667214 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 7.03 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1907758 1 8.49
CHEMBL1824055 1 8.28
CHEMBL3350912 1 8.19
CHEMBL3350911 1 7.99
CHEMBL3350895 1 7.89
CHEMBL3350897 1 7.68
CHEMBL452157 1 7.57
CHEMBL3350898 1 7.57
CHEMBL3350885 1 7.31
CHEMBL3350910 1 7.26
CHEMBL3350908 1 7.06
CHEMBL3350890 1 7.00
CHEMBL3350881 1 6.93
CHEMBL3350899 1 6.67
CHEMBL3350894 1 6.57
CHEMBL2371059 1 6.49
CHEMBL3350905 1 6.49
CHEMBL3350884 1 6.48
CHEMBL3350891 1 6.46
CHEMBL3350724 1 6.40
CHEMBL3350886 1 6.35
CHEMBL3350893 1 6.29
CHEMBL3350900 1 6.19
CHEMBL3350904 1 6.12
CHEMBL3350892 1 6.08
CHEMBL3350887 1 -
CHEMBL3350882 1 -
CHEMBL3350909 1 -
CHEMBL1450103 1 -
CHEMBL3350726 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1907758 IC50 = 3.2 nM 8.49
CHEMBL1824055 IC50 = 5.3 nM 8.28
CHEMBL3350912 IC50 = 6.5 nM 8.19
CHEMBL3350911 IC50 = 10.3 nM 7.99
CHEMBL3350895 IC50 = 13.0 nM 7.89
CHEMBL3350897 IC50 = 21.0 nM 7.68
CHEMBL452157 IC50 = 27.0 nM 7.57
CHEMBL3350898 IC50 = 27.0 nM 7.57
CHEMBL3350885 IC50 = 49.0 nM 7.31
CHEMBL3350910 IC50 = 55.0 nM 7.26
CHEMBL3350908 IC50 = 88.0 nM 7.06
CHEMBL3350890 IC50 = 99.0 nM 7.00
CHEMBL3350881 IC50 = 117.0 nM 6.93
CHEMBL3350899 IC50 = 213.0 nM 6.67
CHEMBL3350894 IC50 = 270.0 nM 6.57
CHEMBL2371059 IC50 = 323.0 nM 6.49
CHEMBL3350905 IC50 = 327.0 nM 6.49
CHEMBL3350884 IC50 = 330.0 nM 6.48
CHEMBL3350891 IC50 = 347.0 nM 6.46
CHEMBL3350724 IC50 = 397.0 nM 6.40
CHEMBL3350886 IC50 = 450.0 nM 6.35
CHEMBL3350893 IC50 = 517.0 nM 6.29
CHEMBL3350900 IC50 = 650.0 nM 6.19
CHEMBL3350904 IC50 = 757.0 nM 6.12
CHEMBL3350892 IC50 = 840.0 nM 6.08
CHEMBL3350889 IC50 > 1000.0 nM -
CHEMBL3350888 IC50 > 1000.0 nM -
CHEMBL3350725 IC50 > 1000.0 nM -
CHEMBL3350903 IC50 > 1000.0 nM -
CHEMBL3350880 IC50 > 1000.0 nM -
CHEMBL3350883 IC50 > 1000.0 nM -
CHEMBL3350896 IC50 > 1000.0 nM -
CHEMBL3350726 IC50 > 1000.0 nM -
CHEMBL1450103 IC50 > 1000.0 nM -
CHEMBL3350909 IC50 > 1000.0 nM -
CHEMBL3350882 IC50 > 1000.0 nM -
CHEMBL3350887 IC50 > 1000.0 nM -