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Assay Detail

CHEMBL1786302

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

Binding
Inhibition of human PDE4B1 incubated for 10 mins using cAMP and [3H]cAMP substrates
36
Total Activities
36
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

Discovery of selective PDE4B inhibitors.
Naganuma K, Omura A, Maekawara N, Saitoh M, Ohkawa N, Kubota T, Nagumo H, Kodama T, Takemura M, Ohtsuka Y, Nakamura J, Tsujita R, Kawasaki K, Yokoi H, Kawanishi M.
Bioorg Med Chem Lett (2009) 19 : 3174 -3176
PubMed 19447034 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.70 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1782307 1 8.17
CHEMBL1782308 1 7.82
CHEMBL1782306 1 7.82
CHEMBL1782305 1 7.72
CHEMBL1782304 1 7.47
CHEMBL1784118 1 7.47
CHEMBL511115 CILOMILAST 3.0 1 7.43
CHEMBL1782290 1 7.17
CHEMBL1782298 1 7.11
CHEMBL1784114 1 6.92
CHEMBL1782289 1 6.92
CHEMBL1784109 1 6.85
CHEMBL1782297 1 6.82
CHEMBL1784107 1 6.72
CHEMBL1782303 1 6.72
CHEMBL1782295 1 6.68
CHEMBL1782294 1 6.66
CHEMBL1782296 1 6.66
CHEMBL1784116 1 6.52
CHEMBL1782286 1 6.50
CHEMBL1784108 1 6.37
CHEMBL1784117 1 6.27
CHEMBL1782302 1 6.22
CHEMBL1782288 1 6.16
CHEMBL1782293 1 6.07
CHEMBL1782300 1 6.03
CHEMBL1782301 1 5.92
CHEMBL1784110 1 5.89
CHEMBL1782299 1 5.75
CHEMBL1782291 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1782307 IC50 = 6.8 nM 8.17
CHEMBL1782308 IC50 = 15.0 nM 7.82
CHEMBL1782306 IC50 = 15.0 nM 7.82
CHEMBL1782305 IC50 = 19.0 nM 7.72
CHEMBL1782304 IC50 = 34.0 nM 7.47
CHEMBL1784118 IC50 = 34.0 nM 7.47
CHEMBL511115 CILOMILAST IC50 = 37.0 nM 7.43
CHEMBL1782290 IC50 = 68.0 nM 7.17
CHEMBL1782298 IC50 = 78.0 nM 7.11
CHEMBL1782289 IC50 = 120.0 nM 6.92
CHEMBL1784114 IC50 = 120.0 nM 6.92
CHEMBL1784109 IC50 = 140.0 nM 6.85
CHEMBL1782297 IC50 = 150.0 nM 6.82
CHEMBL1784107 IC50 = 190.0 nM 6.72
CHEMBL1782303 IC50 = 190.0 nM 6.72
CHEMBL1782295 IC50 = 210.0 nM 6.68
CHEMBL1782294 IC50 = 220.0 nM 6.66
CHEMBL1782296 IC50 = 220.0 nM 6.66
CHEMBL1784116 IC50 = 300.0 nM 6.52
CHEMBL1782286 IC50 = 320.0 nM 6.50
CHEMBL1784108 IC50 = 430.0 nM 6.37
CHEMBL1784117 IC50 = 540.0 nM 6.27
CHEMBL1782302 IC50 = 600.0 nM 6.22
CHEMBL1782288 IC50 = 690.0 nM 6.16
CHEMBL1782293 IC50 = 860.0 nM 6.07
CHEMBL1782300 IC50 = 940.0 nM 6.03
CHEMBL1782301 IC50 = 1200.0 nM 5.92
CHEMBL1784110 IC50 = 1300.0 nM 5.89
CHEMBL1782299 IC50 = 1800.0 nM 5.75
CHEMBL1782291 IC50 = 2800.0 nM 5.55
CHEMBL1782292 IC50 = 3700.0 nM 5.43
CHEMBL1784115 IC50 > 1000.0 nM -
CHEMBL1784113 IC50 > 1000.0 nM -
CHEMBL1784112 IC50 > 1000.0 nM -
CHEMBL1784111 IC50 > 1000.0 nM -
CHEMBL1782287 IC50 > 1000.0 nM -