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Assay Detail

CHEMBL732797

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Binding
Concentration required for in vitro acid stability with hydrochloric acid solution (pH 2.5 ) at room temperature for 2 hr by assaying the solution for motilin receptor binding
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Motilin receptor (CHEMBL5306)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Potent, acid-stable and orally active macrolide-type motilin receptor agonists, GM-611 and the derivatives
Koga H, Sato T, Tsuzuki K, Onoda H, Kuboniwa H, Takanashi H
Bioorg Med Chem Lett (1994) 4 : 1347 -1352
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.35 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL265495 1 8.19
CHEMBL27424 1 8.10
CHEMBL27419 1 8.05
CHEMBL406517 1 7.15
CHEMBL281952 1 6.77
CHEMBL300004 1 6.65
CHEMBL26966 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL265495 IC50 = 6.457 nM 8.19
CHEMBL27424 IC50 = 7.943 nM 8.10
CHEMBL27419 IC50 = 8.913 nM 8.05
CHEMBL406517 IC50 = 70.79 nM 7.15
CHEMBL281952 IC50 = 169.82 nM 6.77
CHEMBL300004 IC50 = 223.87 nM 6.65
CHEMBL26966 IC50 = 302.0 nM 6.52