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Assay Detail

CHEMBL2015744

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

Binding
Binding affinity to human sst5 by in vitro receptor autoradiography assay
9
Total Activities
9
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 5 (CHEMBL1792)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-Methylated sst2 Selective Somatostatin Cyclic Peptide Analogue as a Potent Candidate for Treating Neurogenic Inflammation.
Chatterjee J, Laufer B, Beck JG, Helyes Z, Pintér E, Szolcsányi J, Horvath A, Mandl J, Reubi JC, Kéri G, Kessler H.
ACS Med Chem Lett (2011) 2 : 509 -514
PubMed 24900340 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.09 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL442494 1 8.68
CHEMBL2011463 1 7.28
CHEMBL2011461 1 7.12
CHEMBL311695 SEGLITIDE 2.0 1 7.09
CHEMBL2011462 1 6.90
CHEMBL2011466 1 6.86
CHEMBL2011465 1 6.71
CHEMBL2011464 1 6.61
CHEMBL2011467 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL442494 IC50 = 2.1 nM 8.68
CHEMBL2011463 IC50 = 53.0 nM 7.28
CHEMBL2011461 IC50 = 76.0 nM 7.12
CHEMBL311695 SEGLITIDE IC50 = 81.0 nM 7.09
CHEMBL2011462 IC50 = 126.0 nM 6.90
CHEMBL2011466 IC50 = 137.0 nM 6.86
CHEMBL2011465 IC50 = 196.0 nM 6.71
CHEMBL2011464 IC50 = 247.0 nM 6.61
CHEMBL2011467 IC50 = 263.0 nM 6.58