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Assay Detail

CHEMBL2406782

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

Binding
Inhibition of human full length PDE7A1 expressed in baculovirus infected sf21 cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
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

Discovery of triazines as potent, selective and orally active PDE4 inhibitors.
Gewald R, Grunwald C, Egerland U.
Bioorg Med Chem Lett (2013) 23 : 4308 -4314
PubMed 23806553 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.37 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2402520 1 7.34
CHEMBL2402519 1 6.28
CHEMBL2402517 1 6.27
CHEMBL2402527 1 5.98
CHEMBL2402532 1 5.97
CHEMBL2402358 1 -
CHEMBL2402530 1 -
CHEMBL2402529 1 -
CHEMBL2402526 1 -
CHEMBL2402525 1 -
CHEMBL2402524 1 -
CHEMBL2402523 1 -
CHEMBL2402521 1 -
CHEMBL2402522 1 -
CHEMBL2402518 1 -
CHEMBL2402359 1 -
CHEMBL2402528 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2402520 IC50 = 46.0 nM 7.34
CHEMBL2402519 IC50 = 521.0 nM 6.28
CHEMBL2402517 IC50 = 539.0 nM 6.27
CHEMBL2402527 IC50 = 1050.0 nM 5.98
CHEMBL2402532 IC50 = 1070.0 nM 5.97
CHEMBL2402358 IC50 > 5000.0 nM -
CHEMBL2402530 IC50 > 5000.0 nM -
CHEMBL2402529 IC50 > 5000.0 nM -
CHEMBL2402526 IC50 > 5000.0 nM -
CHEMBL2402525 IC50 > 5000.0 nM -
CHEMBL2402524 IC50 > 5000.0 nM -
CHEMBL2402523 IC50 > 5000.0 nM -
CHEMBL2402521 IC50 - -
CHEMBL2402522 IC50 > 1000.0 nM -
CHEMBL2402518 IC50 > 1000.0 nM -
CHEMBL2402359 IC50 > 5000.0 nM -
CHEMBL2402528 IC50 > 1000.0 nM -