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Assay Detail

CHEMBL1918965

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

Binding
Inhibition of recombinant human PDE7A using [3H]cAMP after 1 hr by scintillation proximity assay
19
Total Activities
19
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

Highly potent, selective, and orally active phosphodiesterase 10A inhibitors.
Malamas MS, Ni Y, Erdei J, Stange H, Schindler R, Lankau HJ, Grunwald C, Fan KY, Parris K, Langen B, Egerland U, Hage T, Marquis KL, Grauer S, Brennan J, Navarra R, Graf R, Harrison BL, Robichaud A, Kronbach T, Pangalos MN, Hoefgen N, Brandon NJ.
J Med Chem (2011) 54 : 7621 -7638
PubMed 21988093 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.98 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1915906 1 6.58
CHEMBL1915891 1 6.48
CHEMBL1915888 1 6.27
CHEMBL1915912 1 6.08
CHEMBL1916106 1 6.04
CHEMBL1915910 1 5.93
CHEMBL1915892 1 5.89
CHEMBL1916108 1 5.87
CHEMBL1916091 1 5.63
CHEMBL1915896 1 5.53
CHEMBL1086110 1 5.48
CHEMBL1916113 1 -
CHEMBL1916114 1 -
CHEMBL1916123 1 -
CHEMBL1916124 1 -
CHEMBL1916125 1 -
CHEMBL1916130 1 -
CHEMBL1916131 1 -
CHEMBL1916132 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1915906 IC50 = 266.0 nM 6.58
CHEMBL1915891 IC50 = 332.0 nM 6.48
CHEMBL1915888 IC50 = 542.0 nM 6.27
CHEMBL1915912 IC50 = 824.0 nM 6.08
CHEMBL1916106 IC50 = 919.0 nM 6.04
CHEMBL1915910 IC50 = 1170.0 nM 5.93
CHEMBL1915892 IC50 = 1300.0 nM 5.89
CHEMBL1916108 IC50 = 1340.0 nM 5.87
CHEMBL1916091 IC50 = 2318.0 nM 5.63
CHEMBL1915896 IC50 = 2930.0 nM 5.53
CHEMBL1086110 IC50 = 3345.0 nM 5.48
CHEMBL1916113 IC50 > 100000.0 nM -
CHEMBL1916114 IC50 > 10000.0 nM -
CHEMBL1916123 IC50 > 10000.0 nM -
CHEMBL1916124 IC50 > 10000.0 nM -
CHEMBL1916125 IC50 > 10000.0 nM -
CHEMBL1916130 IC50 > 500.0 nM -
CHEMBL1916131 IC50 > 1000.0 nM -
CHEMBL1916132 IC50 > 1000.0 nM -