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Assay Detail

CHEMBL5097371

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

Functional
Induction of glucose-stimulated insulin secretion in rat INS-1 832/13 cells incubated for 5 mins by ELISA assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type INS1(832/13)
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

FFAR1/GPR40: One target, different binding sites, many agonists, no drugs, but a continuous and unprofitable tug-of-war between ligand lipophilicity, activity, and toxicity.
Governa P, Caroleo MC, Carullo G, Aiello F, Cione E, Manetti F.
Bioorg Med Chem Lett (2021) 41 : 127969 -127969
PubMed 33771587 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 8.22 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL264374 BEZAFIBRATE 3.0 1 8.22
CHEMBL18901 EFAPROXIRAL 3.0 1 8.22
CHEMBL1201375 TAZAROTENIC ACID -1.0 1 8.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL264374 BEZAFIBRATE EC50 = 6.0 nM 8.22
CHEMBL18901 EFAPROXIRAL EC50 = 6.0 nM 8.22
CHEMBL1201375 TAZAROTENIC ACID EC50 = 6.0 nM 8.22