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Assay Detail

CHEMBL840089

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

Binding
Inhibition of [3H]cAMP binding to recombinant human Phosphodiesterase 4AL (PDE4AL) in baculovirus expression system
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

3',5'-cyclic-AMP phosphodiesterase 4A (CHEMBL254)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyl-adenine: highly potent and selective PDE4 inhibitors.
Whitehead JW, Lee GP, Gharagozloo P, Hofer P, Gehrig A, Wintergerst P, Smyth D, McCoull W, Hachicha M, Patel A, Kyle DJ.
J Med Chem (2005) 48 : 1237 -1243
PubMed 15715490 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 6.41 6.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL362175 1 6.99
CHEMBL368696 1 6.95
CHEMBL180015 1 6.90
CHEMBL360527 1 6.86
CHEMBL367846 1 6.83
CHEMBL178801 1 6.81
CHEMBL433774 1 6.78
CHEMBL360481 1 6.76
CHEMBL433761 1 6.76
CHEMBL1203921 1 6.75
CHEMBL360770 1 6.69
CHEMBL361201 1 6.68
CHEMBL178712 1 6.65
CHEMBL179321 1 6.65
CHEMBL433757 1 6.63
CHEMBL369134 1 6.61
CHEMBL178460 1 6.57
CHEMBL368739 1 6.51
CHEMBL178099 1 6.39
CHEMBL360932 1 6.38
CHEMBL361104 1 5.47
CHEMBL362652 1 5.41
CHEMBL444808 1 5.28
CHEMBL63 ROLIPRAM 2.0 1 5.10
CHEMBL179868 1 4.82
CHEMBL440593 CI-930 1 -
CHEMBL28079 ZAPRINAST 2.0 1 -
CHEMBL434332 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL362175 Ki = 103.0 nM 6.99
CHEMBL368696 Ki = 113.0 nM 6.95
CHEMBL180015 Ki = 126.0 nM 6.90
CHEMBL360527 Ki = 137.0 nM 6.86
CHEMBL367846 Ki = 147.0 nM 6.83
CHEMBL178801 Ki = 155.0 nM 6.81
CHEMBL433774 Ki = 166.0 nM 6.78
CHEMBL360481 Ki = 175.0 nM 6.76
CHEMBL433761 Ki = 175.0 nM 6.76
CHEMBL1203921 Ki = 179.0 nM 6.75
CHEMBL360770 Ki = 206.0 nM 6.69
CHEMBL361201 Ki = 208.0 nM 6.68
CHEMBL178712 Ki = 225.0 nM 6.65
CHEMBL179321 Ki = 223.0 nM 6.65
CHEMBL433757 Ki = 236.0 nM 6.63
CHEMBL369134 Ki = 244.0 nM 6.61
CHEMBL178460 Ki = 271.0 nM 6.57
CHEMBL368739 Ki = 309.0 nM 6.51
CHEMBL178099 Ki = 405.0 nM 6.39
CHEMBL360932 Ki = 415.0 nM 6.38
CHEMBL361104 Ki = 3390.0 nM 5.47
CHEMBL362652 Ki = 3900.0 nM 5.41
CHEMBL444808 Ki = 5200.0 nM 5.28
CHEMBL63 ROLIPRAM Ki = 7940.0 nM 5.10
CHEMBL179868 Ki = 15200.0 nM 4.82
CHEMBL440593 CI-930 Ki > 50000.0 nM -
CHEMBL28079 ZAPRINAST Ki > 50000.0 nM -
CHEMBL434332 Ki > 50000.0 nM -