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Assay Detail

CHEMBL3375768

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

Binding
Displacement of [125I]human ghrelin from mouse GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Identification, optimization, and pharmacology of acylurea GHS-R1a inverse agonists.
McCoull W, Barton P, Brown AJ, Bowker SS, Cameron J, Clarke DS, Davies RD, Dossetter AG, Ertan A, Fenwick M, Green C, Holmes JL, Martin N, Masters D, Moore JE, Newcombe NJ, Newton C, Pointon H, Robb GR, Sheldon C, Stokes S, Morgan D.
J Med Chem (2014) 57 : 6128 -6140
PubMed 24967667 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.23 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3319223 1 8.96
CHEMBL3319215 1 8.31
CHEMBL3319405 1 7.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3319223 IC50 = 1.1 nM 8.96
CHEMBL3319215 IC50 = 4.9 nM 8.31
CHEMBL3319405 IC50 = 39.0 nM 7.41