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Assay Detail

CHEMBL807063

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Binding
Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
21
Total Activities
21
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 5 (CHEMBL1792)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel sst(4)-selective somatostatin (SRIF) agonists. 2. Analogues with beta-methyl-3-(2-naphthyl)alanine substitutions at position 8.
Erchegyi J, Penke B, Simon L, Michaelson S, Wenger S, Waser B, Cescato R, Schaer JC, Reubi JC, Rivier J.
J Med Chem (2003) 46 : 5587 -5596
PubMed 14667213 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.30 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1907758 1 8.54
CHEMBL2371085 1 8.05
CHEMBL2371060 1 7.89
CHEMBL2111257 1 7.76
CHEMBL406373 1 7.64
CHEMBL415582 1 7.57
CHEMBL2371051 1 7.47
CHEMBL415585 1 7.33
CHEMBL263306 1 7.00
CHEMBL415359 1 6.90
CHEMBL2111200 1 6.83
CHEMBL414446 1 6.82
CHEMBL3350357 1 6.17
CHEMBL387458 1 6.16
CHEMBL261895 1 -
CHEMBL410184 1 -
CHEMBL407649 1 -
CHEMBL262975 1 -
CHEMBL1450103 1 -
CHEMBL264046 1 -
CHEMBL414544 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1907758 IC50 = 2.9 nM 8.54
CHEMBL2371085 IC50 = 9.0 nM 8.05
CHEMBL2371060 IC50 = 13.0 nM 7.89
CHEMBL2111257 IC50 = 17.5 nM 7.76
CHEMBL406373 IC50 = 23.0 nM 7.64
CHEMBL415582 IC50 = 27.0 nM 7.57
CHEMBL2371051 IC50 = 34.0 nM 7.47
CHEMBL415585 IC50 = 47.0 nM 7.33
CHEMBL263306 IC50 = 101.0 nM 7.00
CHEMBL415359 IC50 = 127.0 nM 6.90
CHEMBL2111200 IC50 = 147.0 nM 6.83
CHEMBL414446 IC50 = 152.0 nM 6.82
CHEMBL3350357 IC50 = 668.0 nM 6.17
CHEMBL387458 IC50 = 700.0 nM 6.16
CHEMBL261895 IC50 > 1000.0 nM -
CHEMBL410184 IC50 > 1000.0 nM -
CHEMBL407649 IC50 > 1000.0 nM -
CHEMBL262975 IC50 > 10000.0 nM -
CHEMBL1450103 IC50 > 10000.0 nM -
CHEMBL264046 IC50 > 10000.0 nM -
CHEMBL414544 IC50 > 1000.0 nM -