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Assay Detail

CHEMBL4397905

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

Binding
Inhibition of PDE4 in human PBMC assessed as reduction in LPS-stimulated TNFalpha production preincubated for 1 hr followed by LPS stimulation and measured after 18 to 20 hrs by ELISA
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Structure-Aided Identification and Optimization of Tetrahydro-isoquinolines as Novel PDE4 Inhibitors Leading to Discovery of an Effective Antipsoriasis Agent.
Zhang X, Dong G, Li H, Chen W, Li J, Feng C, Gu Z, Zhu F, Zhang R, Li M, Tang W, Liu H, Xu Y.
J Med Chem (2019) 62 : 5579 -5593
PubMed 31099559 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.64 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4527894 1 6.19
CHEMBL4443701 1 5.67
CHEMBL4536368 1 5.59
CHEMBL4543264 1 5.57
CHEMBL4520636 1 5.56
CHEMBL4592339 1 5.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4527894 IC50 = 650.0 nM 6.19
CHEMBL4443701 IC50 = 2160.0 nM 5.67
CHEMBL4536368 IC50 = 2580.0 nM 5.59
CHEMBL4543264 IC50 = 2710.0 nM 5.57
CHEMBL4520636 IC50 = 2730.0 nM 5.56
CHEMBL4592339 IC50 = 5830.0 nM 5.23