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Assay Detail

CHEMBL2173092

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Functional
Agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type COS 7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

An aromatic region to induce a switch between agonism and inverse agonism at the ghrelin receptor.
Els S, Schild E, Petersen PS, Kilian TM, Mokrosinski J, Frimurer TM, Chollet C, Schwartz TW, Holst B, Beck-Sickinger AG.
J Med Chem (2012) 55 : 7437 -7449
PubMed 22920150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 8.17 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL500468 GHRELIN 3.0 1 8.85
CHEMBL2170779 1 7.90
CHEMBL2170780 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL500468 GHRELIN EC50 = 1.4 nM 8.85
CHEMBL2170779 EC50 = 12.6 nM 7.90
CHEMBL2170780 EC50 = 17.9 nM 7.75