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Assay Detail

CHEMBL5330770

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

Binding
Agonist activity at rat GPR35 expressed in HEK293 cells co-expressing Galpha16 assessed as increase in calcium mobilization by Fluo-4 AM dye based fluorescence assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of a novel GPR35 agonist with high and equipotent species potency for oral treatment of IBD.
Song Z, Lu D, Sun J, Ye Y, Fang J, Wang K, Guo S, Zhang Q, He X, Xie X, Shen J.
Bioorg Med Chem (2023) 96 : 117511 -117511
PubMed 37976806 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 7.18 7.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1201266 LODOXAMIDE 4.0 1 7.67
CHEMBL5430512 1 7.46
CHEMBL5437161 1 7.24
CHEMBL5415083 1 7.20
CHEMBL5423540 1 7.19
CHEMBL3245052 1 7.12
CHEMBL3245030 1 7.11
CHEMBL3245049 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1201266 LODOXAMIDE EC50 = 21.5 nM 7.67
CHEMBL5430512 EC50 = 34.6 nM 7.46
CHEMBL5437161 EC50 = 57.8 nM 7.24
CHEMBL5415083 EC50 = 63.0 nM 7.20
CHEMBL5423540 EC50 = 65.2 nM 7.19
CHEMBL3245052 EC50 = 76.7 nM 7.12
CHEMBL3245030 EC50 = 77.8 nM 7.11
CHEMBL3245049 EC50 = 383.0 nM 6.42