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Assay Detail

CHEMBL831432

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

Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Growth hormone secretagogue receptor type 1 (CHEMBL4616)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of the oxindole growth hormone secretagogues.
Tokunaga T, Hume WE, Nagamine J, Kawamura T, Taiji M, Nagata R.
Bioorg Med Chem Lett (2005) 15 : 1789 -1792
PubMed 15780607 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.24 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL178475 1 10.70
CHEMBL500468 GHRELIN 3.0 1 9.85
CHEMBL180349 1 9.62
CHEMBL361804 1 8.80
CHEMBL360227 1 8.68
CHEMBL369533 1 8.40
CHEMBL182035 1 8.38
CHEMBL180096 1 7.82
CHEMBL181313 1 7.11
CHEMBL359922 1 7.08
CHEMBL180755 1 6.97
CHEMBL181312 1 6.94
CHEMBL183916 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL178475 IC50 = 0.02 nM 10.70
CHEMBL500468 GHRELIN IC50 = 0.14 nM 9.85
CHEMBL180349 IC50 = 0.24 nM 9.62
CHEMBL361804 IC50 = 1.6 nM 8.80
CHEMBL360227 IC50 = 2.1 nM 8.68
CHEMBL369533 IC50 = 4.0 nM 8.40
CHEMBL182035 IC50 = 4.2 nM 8.38
CHEMBL180096 IC50 = 15.0 nM 7.82
CHEMBL181313 IC50 = 77.0 nM 7.11
CHEMBL359922 IC50 = 83.0 nM 7.08
CHEMBL180755 IC50 = 106.0 nM 6.97
CHEMBL181312 IC50 = 116.0 nM 6.94
CHEMBL183916 IC50 = 160.0 nM 6.80