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Assay Detail

CHEMBL5145227

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

Binding
Ex vivo agonist activity at GPR38 in rabbit duodenum muscle tissue assessed as intestinal contractile activity
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Muscle tissue
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure.
Toda N, Shida T, Takano R, Katagiri T, Hirouchi M, Abe M, Soma K, Nakagami Y, Yamazaki M.
Bioorg Med Chem Lett (2022) 59 : 128554 -128554
PubMed 35051575 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 8.15 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL525634 1 9.64
CHEMBL5196819 1 8.32
CHEMBL5201797 1 8.14
CHEMBL5197045 1 7.55
CHEMBL489095 CAMICINAL 3.0 1 7.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL525634 EC50 = 0.23 nM 9.64
CHEMBL5196819 EC50 = 4.8 nM 8.32
CHEMBL5201797 EC50 = 7.3 nM 8.14
CHEMBL5197045 EC50 = 28.0 nM 7.55
CHEMBL489095 CAMICINAL EC50 = 82.6 nM 7.08