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Assay Detail

CHEMBL1001500

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

Binding
Displacement of [125I]motilin from MTL receptor in rabbit duodenum homogenate
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Duodenum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Motilin receptor (CHEMBL5306)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Discovery of novel motilin antagonists: Conversion of tetrapeptide leads to orally available peptidomimetics.
Taka N, Matsuoka H, Sato T, Yoshino H, Imaoka I, Sato H, Kotake K, Kumagai Y, Kamei K, Ozaki K, Higashida A, Kuroki T.
Bioorg Med Chem Lett (2009) 19 : 3426 -3429
PubMed 19481451 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.94 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL496391 1 8.96
CHEMBL496191 1 8.72
CHEMBL496190 1 8.37
CHEMBL502792 1 8.22
CHEMBL497004 1 7.92
CHEMBL526496 1 7.92
CHEMBL495994 1 7.62
CHEMBL496390 1 7.57
CHEMBL496389 1 7.34
CHEMBL524083 1 6.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL496391 IC50 = 1.1 nM 8.96
CHEMBL496191 IC50 = 1.9 nM 8.72
CHEMBL496190 IC50 = 4.3 nM 8.37
CHEMBL502792 IC50 = 6.0 nM 8.22
CHEMBL497004 IC50 = 12.0 nM 7.92
CHEMBL526496 IC50 = 12.0 nM 7.92
CHEMBL495994 IC50 = 24.0 nM 7.62
CHEMBL496390 IC50 = 27.0 nM 7.57
CHEMBL496389 IC50 = 46.0 nM 7.34
CHEMBL524083 IC50 = 185.0 nM 6.73