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Assay Detail

CHEMBL4049254

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

Binding
Inhibition of PDE4 (unknown origin) expressed in HEK293 cells co-expressing PM-AKAR3 assessed as increase in cAMP levels by FRET assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Orally Available Soluble Epoxide Hydrolase/Phosphodiesterase 4 Dual Inhibitor Treats Inflammatory Pain.
Blöcher R, Wagner KM, Gopireddy RR, Harris TR, Wu H, Barnych B, Hwang SH, Xiang YK, Proschak E, Morisseau C, Hammock BD.
J Med Chem (2018) 61 : 3541 -3550
PubMed 29614224 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.72 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4097831 1 8.72
CHEMBL4072536 1 8.41
CHEMBL4083949 1 8.09
CHEMBL4099452 1 6.89
CHEMBL63 ROLIPRAM 2.0 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4097831 EC50 = 1.9 nM 8.72
CHEMBL4072536 EC50 = 3.9 nM 8.41
CHEMBL4083949 EC50 = 8.1 nM 8.09
CHEMBL4099452 EC50 = 128.0 nM 6.89
CHEMBL63 ROLIPRAM EC50 = 340.0 nM 6.47