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Assay Detail

CHEMBL1827862

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

Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst2 receptor in CCL39 cells after 2 hrs by autoradiography
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CCL39
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Somatostatin receptor type 2 (CHEMBL1804)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-imidazolebenzyl-histidine substitution in somatostatin and in its octapeptide analogue modulates receptor selectivity and function.
Erchegyi J, Cescato R, Waser B, Rivier JE, Reubi JC.
J Med Chem (2011) 54 : 5981 -5987
PubMed 21806016 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.86 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1823872 SOMATOSTATIN 3.0 1 9.17
CHEMBL1823873 1 8.96
CHEMBL1824052 1 8.80
CHEMBL1824050 1 8.39
CHEMBL1824051 1 7.82
CHEMBL1824049 1 7.46
CHEMBL452157 1 7.39
CHEMBL1824054 1 6.97
CHEMBL1824055 1 6.89
CHEMBL1824056 1 6.76
CHEMBL1824053 1 -
CHEMBL1824057 1 -
CHEMBL1824058 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1823872 SOMATOSTATIN IC50 = 0.67 nM 9.17
CHEMBL1823873 IC50 = 1.1 nM 8.96
CHEMBL1824052 IC50 = 1.6 nM 8.80
CHEMBL1824050 IC50 = 4.1 nM 8.39
CHEMBL1824051 IC50 = 15.0 nM 7.82
CHEMBL1824049 IC50 = 35.0 nM 7.46
CHEMBL452157 IC50 = 41.0 nM 7.39
CHEMBL1824054 IC50 = 106.0 nM 6.97
CHEMBL1824055 IC50 = 130.0 nM 6.89
CHEMBL1824056 IC50 = 173.0 nM 6.76
CHEMBL1824053 IC50 > 1000.0 nM -
CHEMBL1824057 IC50 > 1000.0 nM -
CHEMBL1824058 IC50 > 1000.0 nM -