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Assay Detail

CHEMBL883283

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

Binding
Antagonistic activity against labelled Bombesin receptor bb2 binding sites in rat cerebral cortex by using [125I]- [Tyr] bombesin in presence of NMB; 6.5-31
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
Ashwood V, Brownhill V, Higginbottom M, Horwell DC, Hughes J, Lewthwaite RA, McKnight AT, Pinnock RD, Pritchard MC, Suman-Chauhan N, Webb C, Williams SC.
Bioorg Med Chem Lett (1998) 8 : 2589 -2594
PubMed 9873586 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.80 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL405908 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL405908 IC50 = 16.0 nM 7.80