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Assay Detail

CHEMBL2320850

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

Binding
Displacement of [125I]-Tyr4-BBN from human GRPR overexpressed in human T47D cells
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type T47D
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Heterobivalent dual-target probe for targeting GRP and Y1 receptors on tumor cells.
Shrivastava A, Wang SH, Raju N, Gierach I, Ding H, Tweedle MF.
Bioorg Med Chem Lett (2013) 23 : 687 -692
PubMed 23265893 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.23 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL437027 BOMBESIN 1.0 1 8.70
CHEMBL2314835 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL437027 BOMBESIN IC50 = 2.0 nM 8.70
CHEMBL2314835 IC50 = 18.0 nM 7.75