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Assay Detail

CHEMBL960834

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

Binding
Inhibition of human recombinant PDE4B by scintillation proximity assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

3',5'-cyclic-AMP phosphodiesterase 4B (CHEMBL275)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Quinolines as a novel structural class of potent and selective PDE4 inhibitors: optimisation for oral administration.
Lunniss CJ, Cooper AW, Eldred CD, Kranz M, Lindvall M, Lucas FS, Neu M, Preston AG, Ranshaw LE, Redgrave AJ, Ed Robinson J, Shipley TJ, Solanke YE, Somers DO, Wiseman JO.
Bioorg Med Chem Lett (2009) 19 : 1380 -1385
PubMed 19195882 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.96 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL473764 1 9.50
CHEMBL193240 ROFLUMILAST 4.0 1 9.40
CHEMBL473560 1 9.40
CHEMBL515240 1 8.80
CHEMBL517766 1 8.60
CHEMBL462150 1 8.40
CHEMBL515098 1 8.30
CHEMBL517590 1 8.20
CHEMBL463417 1 7.80
CHEMBL463418 1 7.70
CHEMBL461111 1 7.50
CHEMBL464009 1 7.10
CHEMBL517900 1 7.00
CHEMBL464207 1 7.00
CHEMBL473550 1 6.60
CHEMBL514940 1 6.30
CHEMBL472958 1 6.00
CHEMBL514301 1 5.50
CHEMBL461989 1 5.50
CHEMBL464615 1 5.30
CHEMBL473355 1 5.10
CHEMBL473551 1 4.90
CHEMBL473153 1 4.80
CHEMBL461990 1 4.70
CHEMBL473152 1 4.70
CHEMBL462152 1 -
CHEMBL462151 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL473764 IC50 = 0.3162 nM 9.50
CHEMBL193240 ROFLUMILAST IC50 = 0.3981 nM 9.40
CHEMBL473560 IC50 = 0.3981 nM 9.40
CHEMBL515240 IC50 = 1.585 nM 8.80
CHEMBL517766 IC50 = 2.512 nM 8.60
CHEMBL462150 IC50 = 3.981 nM 8.40
CHEMBL515098 IC50 = 5.012 nM 8.30
CHEMBL517590 IC50 = 6.31 nM 8.20
CHEMBL463417 IC50 = 15.85 nM 7.80
CHEMBL463418 IC50 = 19.95 nM 7.70
CHEMBL461111 IC50 = 31.62 nM 7.50
CHEMBL464009 IC50 = 79.43 nM 7.10
CHEMBL517900 IC50 = 100.0 nM 7.00
CHEMBL464207 IC50 = 100.0 nM 7.00
CHEMBL473550 IC50 = 251.19 nM 6.60
CHEMBL514940 IC50 = 501.19 nM 6.30
CHEMBL472958 IC50 = 1000.0 nM 6.00
CHEMBL514301 IC50 = 3162.28 nM 5.50
CHEMBL461989 IC50 = 3162.28 nM 5.50
CHEMBL464615 IC50 = 5011.87 nM 5.30
CHEMBL473355 IC50 = 7943.28 nM 5.10
CHEMBL473551 IC50 = 12589.25 nM 4.90
CHEMBL473153 IC50 = 15848.93 nM 4.80
CHEMBL461990 IC50 = 19952.62 nM 4.70
CHEMBL473152 IC50 = 19952.62 nM 4.70
CHEMBL462152 IC50 > 31622.78 nM -
CHEMBL462151 IC50 > 31622.78 nM -