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Assay Detail

CHEMBL803844

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

Binding
Binding affinity for SSTR2 receptors of rat cortex membranes was determined by using [125I][Tyr3]-octreotide radioligand
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Direct synthesis of [DOTA-DPhe1]-octreotide and [DOTA-DPhe1,Tyr3]-octreotide (SMT487): two conjugates for systemic delivery of radiotherapeutical nuclides to somatostatin receptor positive tumors in man.
Albert R, Smith-Jones P, Stolz B, Simeon C, Knecht H, Bruns C, Pless J.
Bioorg Med Chem Lett (1998) 8 : 1207 -1210
PubMed 9871736 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 8.90 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3350037 1 9.30
CHEMBL410194 1 8.90
CHEMBL407643 1 8.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3350037 Ki = 0.5012 nM 9.30
CHEMBL410194 Ki = 1.259 nM 8.90
CHEMBL407643 Ki = 3.162 nM 8.50