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Assay Detail

CHEMBL768860

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Binding
Inhibitory potency against pig aortic PDE IV
ChEMBL ↗
71
Total Activities
69
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Phosphodiesterase 4A (CHEMBL3333) ↗
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues.
Ashton MJ, Cook DC, Fenton G, Karlsson JA, Palfreyman MN, Raeburn D, Ratcliffe AJ, Souness JE, Thurairatnam S, Vicker N.
J Med Chem (1994) 37 : 1696 -1703
PubMed 8201604 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 71 6.59 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42126 PICLAMILAST 2.0 1 9.00
CHEMBL296477 — — 3 9.00
CHEMBL45395 — — 1 8.70
CHEMBL46142 — — 1 8.15
CHEMBL297555 — — 1 8.10
CHEMBL300290 — — 1 8.00
CHEMBL295976 — — 1 7.80
CHEMBL298262 — — 1 7.70
CHEMBL45834 — — 1 7.64
CHEMBL44790 — — 1 7.46
CHEMBL296789 — — 1 7.30
CHEMBL300661 — — 1 7.16
CHEMBL47113 — — 1 7.16
CHEMBL47770 — — 1 7.07
CHEMBL294949 — — 1 7.00
CHEMBL48017 — — 1 7.00
CHEMBL295669 — — 1 7.00
CHEMBL47286 — — 1 7.00
CHEMBL48048 — — 1 6.92
CHEMBL296700 — — 1 6.89
CHEMBL289190 — — 1 6.72
CHEMBL45359 — — 1 6.70
CHEMBL47288 — — 1 6.70
CHEMBL45128 — — 1 6.62
CHEMBL45687 — — 1 6.60
CHEMBL45738 — — 1 6.60
CHEMBL431146 — — 1 6.52
CHEMBL44629 — — 1 6.52
CHEMBL441431 — — 1 6.44
CHEMBL46044 — — 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296477 — IC50 = 1.0 nM 9.00
CHEMBL296477 — IC50 = 1.0 nM 9.00
CHEMBL296477 — IC50 = 1.0 nM 9.00
CHEMBL42126 PICLAMILAST IC50 = 1.0 nM 9.00
CHEMBL45395 — IC50 = 2.0 nM 8.70
CHEMBL46142 — IC50 = 7.0 nM 8.15
CHEMBL297555 — IC50 = 8.0 nM 8.10
CHEMBL300290 — IC50 = 10.0 nM 8.00
CHEMBL295976 — IC50 = 16.0 nM 7.80
CHEMBL298262 — IC50 = 20.0 nM 7.70
CHEMBL45834 — IC50 = 23.0 nM 7.64
CHEMBL44790 — IC50 = 35.0 nM 7.46
CHEMBL296789 — IC50 = 50.0 nM 7.30
CHEMBL47113 — IC50 = 70.0 nM 7.16
CHEMBL300661 — IC50 = 70.0 nM 7.16
CHEMBL47770 — IC50 = 85.0 nM 7.07
CHEMBL47286 — IC50 = 100.0 nM 7.00
CHEMBL295669 — IC50 = 100.0 nM 7.00
CHEMBL48017 — IC50 = 100.0 nM 7.00
CHEMBL294949 — IC50 = 100.0 nM 7.00
CHEMBL48048 — IC50 = 120.0 nM 6.92
CHEMBL296700 — IC50 = 130.0 nM 6.89
CHEMBL289190 — IC50 = 190.0 nM 6.72
CHEMBL45359 — IC50 = 200.0 nM 6.70
CHEMBL47288 — IC50 = 200.0 nM 6.70
CHEMBL45128 — IC50 = 240.0 nM 6.62
CHEMBL45738 — IC50 = 250.0 nM 6.60
CHEMBL45687 — IC50 = 250.0 nM 6.60
CHEMBL431146 — IC50 = 300.0 nM 6.52
CHEMBL44629 — IC50 = 300.0 nM 6.52
CHEMBL441431 — IC50 = 360.0 nM 6.44
CHEMBL298792 — IC50 = 400.0 nM 6.40
CHEMBL46044 — IC50 = 400.0 nM 6.40
CHEMBL45055 — IC50 = 400.0 nM 6.40
CHEMBL50012 — IC50 = 450.0 nM 6.35
CHEMBL297149 — IC50 = 500.0 nM 6.30
CHEMBL44673 — IC50 = 500.0 nM 6.30
CHEMBL298426 — IC50 = 500.0 nM 6.30
CHEMBL296882 — IC50 = 550.0 nM 6.26
CHEMBL301813 — IC50 = 550.0 nM 6.26
CHEMBL45854 — IC50 = 650.0 nM 6.19
CHEMBL296799 — IC50 = 800.0 nM 6.10
CHEMBL297333 — IC50 = 900.0 nM 6.05
CHEMBL47841 — IC50 = 1000.0 nM 6.00
CHEMBL296575 — IC50 = 1000.0 nM 6.00
CHEMBL47957 — IC50 = 1200.0 nM 5.92
CHEMBL45231 — IC50 = 1200.0 nM 5.92
CHEMBL48080 — IC50 = 1300.0 nM 5.89
CHEMBL416466 — IC50 = 1300.0 nM 5.89
CHEMBL298000 — IC50 = 1600.0 nM 5.80