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Assay Detail

CHEMBL831870

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

Binding
Displacement of [125 I-Tyr4]BB from human gastrin releasing peptide receptor expressed in PC-3 cell membranes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PC-3
Confidence 9 — Direct single protein target
Curated By Expert

Target

Gastrin-releasing peptide receptor (CHEMBL4959)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent bombesin-like peptides for GRP-receptor targeting of tumors with 99mTc: a preclinical study.
Nock BA, Nikolopoulou A, Galanis A, Cordopatis P, Waser B, Reubi JC, Maina T.
J Med Chem (2005) 48 : 100 -110
PubMed 15634004 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 9.69 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2371725 Demobesin 3 1 10.22
CHEMBL414307 1 10.10
CHEMBL2371724 1 9.82
CHEMBL266079 1 9.22
CHEMBL2371726 1 9.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2371725 Demobesin 3 IC50 = 0.06 nM 10.22
CHEMBL414307 IC50 = 0.08 nM 10.10
CHEMBL2371724 IC50 = 0.15 nM 9.82
CHEMBL266079 IC50 = 0.6 nM 9.22
CHEMBL2371726 IC50 = 0.85 nM 9.07