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Assay Detail

CHEMBL4729136

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

Binding
Agonist activity at zebrafish GPR34 type a expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
6
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Danio rerio
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

G protein-coupled receptor 34a (CHEMBL4739839)
Type SINGLE PROTEIN
Organism Danio rerio

Publication

Non-naturally Occurring Regio Isomer of Lysophosphatidylserine Exhibits Potent Agonistic Activity toward G Protein-Coupled Receptors.
Nakamura S,Sayama M,Uwamizu A,Jung S,Ikubo M,Otani Y,Kano K,Omi J,Inoue A,Aoki J,Ohwada T
J Med Chem (2020) 63 : 9990 -10029
PubMed 32787112 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.59 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1742484 2 6.89
CHEMBL4753103 2 6.29
CHEMBL4758243 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1742484 EC50 = 130.0 nM 6.89
CHEMBL1742484 EC50 = 128.82 nM 6.89
CHEMBL4753103 EC50 = 510.0 nM 6.29
CHEMBL4753103 EC50 = 512.86 nM 6.29
CHEMBL4758243 EC50 > 3000.0 nM -
CHEMBL4758243 EC50 < 3162.28 nM -