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Assay Detail

CHEMBL821513

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

Binding
In vivo inhibition of cyclic AMP phosphodiesterase from human platelets
87
Total Activities
87
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 3 (CHEMBL2094125)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Inhibitors of cyclic AMP phosphodiesterase. 2. Structural variations of N-cyclohexyl-N-methyl-4-[(1,2,3,5-tetrahydro- 2-oxoimidazo[2,1-b]quinazolin-7-yl)-oxy]butyramide (RS-82856).
Venuti MC, Jones GH, Alvarez R, Bruno JJ.
J Med Chem (1987) 30 : 303 -318
PubMed 3027339 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 87 7.12 9.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL326891 1 9.03
CHEMBL108876 1 9.00
CHEMBL321600 1 9.00
CHEMBL109149 1 8.96
CHEMBL324011 1 8.89
CHEMBL107651 1 8.84
CHEMBL110484 1 8.84
CHEMBL106922 1 8.82
CHEMBL106201 1 8.73
CHEMBL322596 1 8.70
CHEMBL110172 1 8.66
CHEMBL110350 1 8.57
CHEMBL108914 1 8.49
CHEMBL109062 1 8.44
CHEMBL107034 1 8.39
CHEMBL110734 1 8.35
CHEMBL109096 1 8.34
CHEMBL108741 1 8.31
CHEMBL110374 1 8.30
CHEMBL106141 1 8.27
CHEMBL110087 1 8.25
CHEMBL320430 1 8.23
CHEMBL110338 1 8.22
CHEMBL107939 1 8.19
CHEMBL419368 1 8.04
CHEMBL105793 1 8.00
CHEMBL110675 1 7.96
CHEMBL109058 1 7.92
CHEMBL262661 1 7.92
CHEMBL320180 1 7.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL326891 IC50 = 0.94 nM 9.03
CHEMBL108876 IC50 = 1.0 nM 9.00
CHEMBL321600 IC50 = 1.0 nM 9.00
CHEMBL109149 IC50 = 1.1 nM 8.96
CHEMBL324011 IC50 = 1.3 nM 8.89
CHEMBL107651 IC50 = 1.45 nM 8.84
CHEMBL110484 IC50 = 1.45 nM 8.84
CHEMBL106922 IC50 = 1.5 nM 8.82
CHEMBL106201 IC50 = 1.85 nM 8.73
CHEMBL322596 IC50 = 2.0 nM 8.70
CHEMBL110172 IC50 = 2.2 nM 8.66
CHEMBL110350 IC50 = 2.7 nM 8.57
CHEMBL108914 IC50 = 3.2 nM 8.49
CHEMBL109062 IC50 = 3.6 nM 8.44
CHEMBL107034 IC50 = 4.1 nM 8.39
CHEMBL110734 IC50 = 4.5 nM 8.35
CHEMBL109096 IC50 = 4.6 nM 8.34
CHEMBL108741 IC50 = 4.9 nM 8.31
CHEMBL110374 IC50 = 5.0 nM 8.30
CHEMBL106141 IC50 = 5.4 nM 8.27
CHEMBL110087 IC50 = 5.6 nM 8.25
CHEMBL320430 IC50 = 5.9 nM 8.23
CHEMBL110338 IC50 = 6.0 nM 8.22
CHEMBL107939 IC50 = 6.4 nM 8.19
CHEMBL419368 IC50 = 9.2 nM 8.04
CHEMBL105793 IC50 = 10.0 nM 8.00
CHEMBL110675 IC50 = 11.0 nM 7.96
CHEMBL109058 IC50 = 12.0 nM 7.92
CHEMBL262661 IC50 = 12.0 nM 7.92
CHEMBL320180 IC50 = 12.5 nM 7.90
CHEMBL108703 IC50 = 13.0 nM 7.89
CHEMBL110450 IC50 = 13.5 nM 7.87
CHEMBL323400 IC50 = 14.0 nM 7.85
CHEMBL110483 IC50 = 15.0 nM 7.82
CHEMBL323174 IC50 = 16.0 nM 7.80
CHEMBL107261 IC50 = 17.0 nM 7.77
CHEMBL108152 IC50 = 18.0 nM 7.75
CHEMBL107937 IC50 = 18.5 nM 7.73
CHEMBL110787 IC50 = 26.0 nM 7.58
CHEMBL430684 IC50 = 26.0 nM 7.58
CHEMBL108913 IC50 = 26.0 nM 7.58
CHEMBL106498 IC50 = 27.5 nM 7.56
CHEMBL432398 IC50 = 48.0 nM 7.32
CHEMBL323494 IC50 = 72.0 nM 7.14
CHEMBL322946 IC50 = 76.0 nM 7.12
CHEMBL109057 IC50 = 120.0 nM 6.92
CHEMBL108365 IC50 = 130.0 nM 6.89
CHEMBL110218 IC50 = 140.0 nM 6.85
CHEMBL108752 IC50 = 150.0 nM 6.82
CHEMBL440593 CI-930 IC50 = 150.0 nM 6.82