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Assay Detail

CHEMBL1920121

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Binding
Inhibition of bovine aortic PDE4 using cAMP as substrate in presence of cGMP
ChEMBL ↗
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam.
Bihel FJ, Justiniano H, Schmitt M, Hellal M, Ibrahim MA, Lugnier C, Bourguignon JJ.
Bioorg Med Chem Lett (2011) 21 : 6567 -6572
PubMed 21920746 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 5.83 7.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1915293 — — 1 7.06
CHEMBL1915295 — — 1 6.85
CHEMBL1915294 — — 1 6.72
CHEMBL1915067 — — 1 6.70
CHEMBL1915292 — — 1 6.58
CHEMBL1915069 — — 1 6.52
CHEMBL1915072 — — 1 6.52
CHEMBL1915066 — — 1 6.41
CHEMBL1555736 ETHAVERINE 2.0 1 6.40
CHEMBL404216 TOFISOPAM 2.0 1 6.17
CHEMBL1915291 — — 1 6.10
CHEMBL1915289 — — 1 6.10
CHEMBL1915301 — — 1 6.07
CHEMBL1915300 — — 1 6.02
CHEMBL19224 PAPAVERINE 3.0 1 5.96
CHEMBL1915071 — — 1 5.92
CHEMBL1915290 — — 1 5.85
CHEMBL1915308 — — 1 5.85
CHEMBL1915070 — — 1 5.82
CHEMBL281610 — — 1 5.82
CHEMBL1915303 — — 1 5.80
CHEMBL1915314 — — 1 5.66
CHEMBL1566493 — — 1 5.64
CHEMBL1915302 — — 1 5.64
CHEMBL1915307 — — 1 5.54
CHEMBL1915065 GIRISOPAM 2.0 1 5.50
CHEMBL1915313 — — 1 5.44
CHEMBL1915311 — — 1 5.37
CHEMBL1915312 — — 1 5.30
CHEMBL280689 — — 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1915293 — IC50 = 87.0 nM 7.06
CHEMBL1915295 — IC50 = 140.0 nM 6.85
CHEMBL1915294 — IC50 = 190.0 nM 6.72
CHEMBL1915067 — IC50 = 200.0 nM 6.70
CHEMBL1915292 — IC50 = 260.0 nM 6.58
CHEMBL1915069 — IC50 = 300.0 nM 6.52
CHEMBL1915072 — IC50 = 300.0 nM 6.52
CHEMBL1915066 — IC50 = 390.0 nM 6.41
CHEMBL1555736 ETHAVERINE IC50 = 400.0 nM 6.40
CHEMBL404216 TOFISOPAM IC50 = 680.0 nM 6.17
CHEMBL1915291 — IC50 = 800.0 nM 6.10
CHEMBL1915289 — IC50 = 800.0 nM 6.10
CHEMBL1915301 — IC50 = 860.0 nM 6.07
CHEMBL1915300 — IC50 = 950.0 nM 6.02
CHEMBL19224 PAPAVERINE IC50 = 1100.0 nM 5.96
CHEMBL1915071 — IC50 = 1200.0 nM 5.92
CHEMBL1915290 — IC50 = 1400.0 nM 5.85
CHEMBL1915308 — IC50 = 1400.0 nM 5.85
CHEMBL1915070 — IC50 = 1500.0 nM 5.82
CHEMBL281610 — IC50 = 1500.0 nM 5.82
CHEMBL1915303 — IC50 = 1600.0 nM 5.80
CHEMBL1915314 — IC50 = 2200.0 nM 5.66
CHEMBL1915302 — IC50 = 2300.0 nM 5.64
CHEMBL1566493 — IC50 = 2300.0 nM 5.64
CHEMBL1915307 — IC50 = 2900.0 nM 5.54
CHEMBL1915065 GIRISOPAM IC50 = 3200.0 nM 5.50
CHEMBL1915313 — IC50 = 3600.0 nM 5.44
CHEMBL1915311 — IC50 = 4300.0 nM 5.37
CHEMBL1915312 — IC50 = 5000.0 nM 5.30
CHEMBL280689 — IC50 = 5100.0 nM 5.29
CHEMBL279064 — IC50 = 7700.0 nM 5.11
CHEMBL1915068 — IC50 = 7700.0 nM 5.11
CHEMBL1915310 — IC50 = 7900.0 nM 5.10
CHEMBL1915304 — IC50 = 8400.0 nM 5.08
CHEMBL477944 — IC50 = 9600.0 nM 5.02
CHEMBL1558214 — IC50 = 17000.0 nM 4.77
CHEMBL1915297 — IC50 = 18000.0 nM 4.75
CHEMBL1915309 — IC50 > 20000.0 nM -
CHEMBL1915298 — IC50 > 20000.0 nM -
CHEMBL1915299 — IC50 > 20000.0 nM -
CHEMBL1915306 — IC50 > 20000.0 nM -
CHEMBL1915305 — IC50 > 20000.0 nM -
CHEMBL1915296 — IC50 > 20000.0 nM -