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Assay Detail

CHEMBL4268301

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

Binding
Inhibition of recombinant human PDE7A using cAMP as substrate after 10 mins by PDE-Glo Phosphodiesterase Assay
26
Total Activities
26
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

High affinity 3',5'-cyclic-AMP phosphodiesterase 7A (CHEMBL3012)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel amide derivatives of 1,3-dimethyl-2,6-dioxopurin-7-yl-alkylcarboxylic acids as multifunctional TRPA1 antagonists and PDE4/7 inhibitors: A new approach for the treatment of pain.
Chłoń-Rzepa G, Ślusarczyk M, Jankowska A, Gawalska A, Bucki A, Kołaczkowski M, Świerczek A, Pociecha K, Wyska E, Zygmunt M, Kazek G, Sałat K, Pawłowski M.
Eur J Med Chem (2018) 158 : 517 -533
PubMed 30245393 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 4.70 5.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL484928 1 5.68
CHEMBL4289050 1 5.29
CHEMBL4284497 1 5.11
CHEMBL4282582 1 5.04
CHEMBL4280337 1 4.70
CHEMBL4292772 1 4.70
CHEMBL4291934 1 4.42
CHEMBL4290956 1 4.39
CHEMBL4290996 1 4.26
CHEMBL275084 ISOBUTYLMETHYLXANTHINE 1 4.07
CHEMBL4288977 1 4.02
CHEMBL63 ROLIPRAM 2.0 1 -
CHEMBL4280678 1 -
CHEMBL4290575 1 -
CHEMBL4294138 1 -
CHEMBL4287148 1 -
CHEMBL4279233 1 -
CHEMBL4283794 1 -
CHEMBL4294370 1 -
CHEMBL4284046 1 -
CHEMBL4290979 1 -
CHEMBL4290814 1 -
CHEMBL4280173 1 -
CHEMBL4287403 1 -
CHEMBL4276743 1 -
CHEMBL1086310 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL484928 IC50 = 2100.0 nM 5.68
CHEMBL4289050 IC50 = 5070.0 nM 5.29
CHEMBL4284497 IC50 = 7760.0 nM 5.11
CHEMBL4282582 IC50 = 9060.0 nM 5.04
CHEMBL4280337 IC50 = 19750.0 nM 4.70
CHEMBL4292772 IC50 = 19960.0 nM 4.70
CHEMBL4291934 IC50 = 37590.0 nM 4.42
CHEMBL4290956 IC50 = 41150.0 nM 4.39
CHEMBL4290996 IC50 = 54280.0 nM 4.26
CHEMBL275084 ISOBUTYLMETHYLXANTHINE IC50 = 85600.0 nM 4.07
CHEMBL4288977 IC50 = 96320.0 nM 4.02
CHEMBL63 ROLIPRAM IC50 > 200000.0 nM -
CHEMBL4280678 IC50 > 200000.0 nM -
CHEMBL4290575 IC50 > 200000.0 nM -
CHEMBL4294138 IC50 > 200000.0 nM -
CHEMBL4287148 IC50 > 200000.0 nM -
CHEMBL4279233 IC50 > 200000.0 nM -
CHEMBL4283794 IC50 > 200000.0 nM -
CHEMBL4294370 IC50 > 200000.0 nM -
CHEMBL4284046 IC50 > 200000.0 nM -
CHEMBL4290979 IC50 > 200000.0 nM -
CHEMBL4290814 IC50 > 200000.0 nM -
CHEMBL4280173 IC50 > 200000.0 nM -
CHEMBL4287403 IC50 > 200000.0 nM -
CHEMBL4276743 IC50 > 200000.0 nM -
CHEMBL1086310 IC50 > 200000.0 nM -