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Assay Detail

CHEMBL4369833

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

Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

N-Terminal Liver-Expressed Antimicrobial Peptide 2 (LEAP2) Region Exhibits Inverse Agonist Activity toward the Ghrelin Receptor.
M'Kadmi C, Cabral A, Barrile F, Giribaldi J, Cantel S, Damian M, Mary S, Denoyelle S, Dutertre S, Péraldi-Roux S, Neasta J, Oiry C, Banères JL, Marie J, Perello M, Fehrentz JA.
J Med Chem (2019) 62 : 965 -973
PubMed 30543423 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 8.28 8.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4517399 1 8.90
CHEMBL425281 1 8.89
CHEMBL4463042 1 8.57
CHEMBL4475293 1 8.52
CHEMBL4456830 1 8.47
CHEMBL4556887 1 8.44
CHEMBL2170781 1 8.43
CHEMBL4541252 1 8.19
CHEMBL4581511 1 7.26
CHEMBL501261 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4517399 Ki = 1.26 nM 8.90
CHEMBL425281 Ki = 1.28 nM 8.89
CHEMBL4463042 Ki = 2.7 nM 8.57
CHEMBL4475293 Ki = 3.05 nM 8.52
CHEMBL4456830 Ki = 3.4 nM 8.47
CHEMBL4556887 Ki = 3.66 nM 8.44
CHEMBL2170781 Ki = 3.7 nM 8.43
CHEMBL4541252 Ki = 6.45 nM 8.19
CHEMBL4581511 Ki = 55.0 nM 7.26
CHEMBL501261 Ki = 76.7 nM 7.12