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Assay Detail

CHEMBL893771

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Binding
Inhibition of PDE4 in U937 cells
17
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U-937
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Dual M3 antagonists-PDE4 inhibitors. Part 2: Synthesis and SAR of 3-substituted azetidinyl derivatives.
Provins L, Christophe B, Danhaive P, Dulieu J, Gillard M, Quéré L, Stebbins K.
Bioorg Med Chem Lett (2007) 17 : 3077 -3080
PubMed 17398090 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.16 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL396761 2 7.30
CHEMBL232417 1 6.70
CHEMBL232419 2 6.60
CHEMBL436814 1 6.30
CHEMBL205654 2 6.20
CHEMBL242822 1 6.20
CHEMBL232416 1 6.10
CHEMBL232860 1 6.10
CHEMBL245137 1 6.00
CHEMBL389992 1 5.70
CHEMBL242823 1 5.70
CHEMBL234099 1 5.50
CHEMBL232208 1 5.40
CHEMBL434388 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL396761 IC50 = 50.12 nM 7.30
CHEMBL396761 IC50 = 79.0 nM 7.10
CHEMBL232417 IC50 = 200.0 nM 6.70
CHEMBL232419 IC50 = 251.19 nM 6.60
CHEMBL232419 IC50 = 320.0 nM 6.50
CHEMBL436814 IC50 = 500.0 nM 6.30
CHEMBL242822 IC50 = 630.0 nM 6.20
CHEMBL205654 IC50 = 630.0 nM 6.20
CHEMBL232416 IC50 = 790.0 nM 6.10
CHEMBL205654 IC50 = 794.33 nM 6.10
CHEMBL232860 IC50 = 790.0 nM 6.10
CHEMBL245137 IC50 = 1000.0 nM 6.00
CHEMBL389992 IC50 = 2000.0 nM 5.70
CHEMBL242823 IC50 = 2000.0 nM 5.70
CHEMBL234099 IC50 = 3200.0 nM 5.50
CHEMBL232208 IC50 = 4000.0 nM 5.40
CHEMBL434388 IC50 = 5000.0 nM 5.30