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Assay Detail

CHEMBL5098801

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

Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Apelin receptor (CHEMBL1628481)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a Hydroxypyrimidinone Compound (<b>21</b>) as a Potent APJ Receptor Agonist for the Potential Treatment of Heart Failure.
Meng W, Pi Z, Brigance R, Rossi KA, Schumacher WA, Bostwick JS, Gargalovic PS, Onorato JM, Luk CE, Generaux CN, Wang T, Wexler RR, Finlay HJ.
J Med Chem (2021) 64 : 18102 -18113
PubMed 34855405 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 10.00 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5193130 1 10.70
CHEMBL5173464 1 10.70
CHEMBL5208127 1 10.70
CHEMBL5192130 1 10.70
CHEMBL5205562 1 10.70
CHEMBL5202635 1 10.70
CHEMBL5175424 1 10.52
CHEMBL5202233 1 10.52
CHEMBL5197398 1 10.40
CHEMBL414173 1 10.30
CHEMBL5170657 1 10.22
CHEMBL5179504 1 10.15
CHEMBL5199079 1 9.70
CHEMBL5184730 1 9.70
CHEMBL5185709 1 9.40
CHEMBL4870497 1 9.40
CHEMBL5206677 1 9.22
CHEMBL5190307 1 8.74
CHEMBL5197115 1 8.72
CHEMBL5190259 1 8.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5193130 EC50 = 0.02 nM 10.70
CHEMBL5173464 EC50 = 0.02 nM 10.70
CHEMBL5208127 EC50 = 0.02 nM 10.70
CHEMBL5192130 EC50 = 0.02 nM 10.70
CHEMBL5205562 EC50 = 0.02 nM 10.70
CHEMBL5202635 EC50 = 0.02 nM 10.70
CHEMBL5175424 EC50 = 0.03 nM 10.52
CHEMBL5202233 EC50 = 0.03 nM 10.52
CHEMBL5197398 EC50 = 0.04 nM 10.40
CHEMBL414173 EC50 = 0.05 nM 10.30
CHEMBL5170657 EC50 = 0.06 nM 10.22
CHEMBL5179504 EC50 = 0.07 nM 10.15
CHEMBL5199079 EC50 = 0.2 nM 9.70
CHEMBL5184730 EC50 = 0.2 nM 9.70
CHEMBL5185709 EC50 = 0.4 nM 9.40
CHEMBL4870497 EC50 = 0.4 nM 9.40
CHEMBL5206677 EC50 = 0.6 nM 9.22
CHEMBL5190307 EC50 = 1.8 nM 8.74
CHEMBL5197115 EC50 = 1.9 nM 8.72
CHEMBL5190259 EC50 = 1.9 nM 8.72