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Assay Detail

CHEMBL828294

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

Binding
Inhibition of human Phosphodiesterase 4D3 expressed in baculovirus infected Sf9 cells
59
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Expert

Target

3',5'-cyclic-AMP phosphodiesterase 4D (CHEMBL288)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: design, synthesis and structure-activity relationship studies.
Vergne F, Bernardelli P, Lorthiois E, Pham N, Proust E, Oliveira C, Mafroud AK, Royer F, Wrigglesworth R, Schellhaas J, Barvian M, Moreau F, Idrissi M, Tertre A, Bertin B, Coupe M, Berna P, Soulard P.
Bioorg Med Chem Lett (2004) 14 : 4607 -4613
PubMed 15324874 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 59 4.64 5.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL185203 1 5.37
CHEMBL263311 1 5.25
CHEMBL186615 1 5.23
CHEMBL184829 1 5.23
CHEMBL182681 1 5.20
CHEMBL184017 1 5.15
CHEMBL184154 1 5.06
CHEMBL183119 1 4.96
CHEMBL365659 1 4.92
CHEMBL185439 1 4.91
CHEMBL361512 1 4.89
CHEMBL182227 1 4.85
CHEMBL185446 1 4.82
CHEMBL184057 1 4.82
CHEMBL369541 1 4.77
CHEMBL182294 1 4.72
CHEMBL184016 1 4.72
CHEMBL183952 1 4.71
CHEMBL363673 1 4.69
CHEMBL185604 1 4.67
CHEMBL367135 1 4.65
CHEMBL359562 1 4.65
CHEMBL360874 1 4.64
CHEMBL185144 1 4.60
CHEMBL362033 1 4.59
CHEMBL363118 1 4.58
CHEMBL183816 1 4.58
CHEMBL184470 1 4.52
CHEMBL365634 1 4.49
CHEMBL187201 1 4.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL185203 IC50 = 4260.0 nM 5.37
CHEMBL263311 IC50 = 5630.0 nM 5.25
CHEMBL184829 IC50 = 5840.0 nM 5.23
CHEMBL186615 IC50 = 5900.0 nM 5.23
CHEMBL182681 IC50 = 6300.0 nM 5.20
CHEMBL184017 IC50 = 7050.0 nM 5.15
CHEMBL184154 IC50 = 8770.0 nM 5.06
CHEMBL183119 IC50 = 10970.0 nM 4.96
CHEMBL365659 IC50 = 11880.0 nM 4.92
CHEMBL185439 IC50 = 12230.0 nM 4.91
CHEMBL361512 IC50 = 13000.0 nM 4.89
CHEMBL182227 IC50 = 14200.0 nM 4.85
CHEMBL185446 IC50 = 15300.0 nM 4.82
CHEMBL184057 IC50 = 15050.0 nM 4.82
CHEMBL369541 IC50 = 17000.0 nM 4.77
CHEMBL182294 IC50 = 19000.0 nM 4.72
CHEMBL184016 IC50 = 19250.0 nM 4.72
CHEMBL183952 IC50 = 19330.0 nM 4.71
CHEMBL363673 IC50 = 20500.0 nM 4.69
CHEMBL185604 IC50 = 21330.0 nM 4.67
CHEMBL367135 IC50 = 22170.0 nM 4.65
CHEMBL359562 IC50 = 22250.0 nM 4.65
CHEMBL360874 IC50 = 23000.0 nM 4.64
CHEMBL185144 IC50 = 25000.0 nM 4.60
CHEMBL362033 IC50 = 25750.0 nM 4.59
CHEMBL363118 IC50 = 26000.0 nM 4.58
CHEMBL183816 IC50 = 26000.0 nM 4.58
CHEMBL184470 IC50 = 30000.0 nM 4.52
CHEMBL365634 IC50 = 32250.0 nM 4.49
CHEMBL187201 IC50 = 33330.0 nM 4.48
CHEMBL363097 IC50 = 34250.0 nM 4.46
CHEMBL363709 IC50 = 36330.0 nM 4.44
CHEMBL363236 IC50 = 37000.0 nM 4.43
CHEMBL184806 IC50 = 38000.0 nM 4.42
CHEMBL360434 IC50 = 40000.0 nM 4.40
CHEMBL182574 IC50 = 39660.0 nM 4.40
CHEMBL184089 IC50 = 44660.0 nM 4.35
CHEMBL184960 IC50 = 44500.0 nM 4.35
CHEMBL184334 IC50 = 57000.0 nM 4.24
CHEMBL184837 IC50 = 58250.0 nM 4.24
CHEMBL361706 IC50 = 71000.0 nM 4.15
CHEMBL185502 IC50 = 79000.0 nM 4.10
CHEMBL182788 IC50 = 81500.0 nM 4.09
CHEMBL186868 IC50 = 92330.0 nM 4.04
CHEMBL362264 IC50 = 95500.0 nM 4.02
CHEMBL365206 IC50 > 101000.0 nM -
CHEMBL185532 IC50 > 101000.0 nM -
CHEMBL185531 IC50 > 101000.0 nM -
CHEMBL365402 IC50 > 101000.0 nM -
CHEMBL185173 IC50 > 101000.0 nM -