Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1058320

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

Binding
Inhibition of PDE6
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Identification, synthesis and SAR of amino substituted pyrido[3,2b]pyrazinones as potent and selective PDE5 inhibitors.
Owen DR, Walker JK, Jon Jacobsen E, Freskos JN, Hughes RO, Brown DL, Bell AS, Brown DG, Phillips C, Mischke BV, Molyneaux JM, Fobian YM, Heasley SE, Moon JB, Stallings WC, Joseph Rogier D, Fox DN, Palmer MJ, Ringer T, Rodriquez-Lens M, Cubbage JW, Blevis-Bal RM, Benson AG, Acker BA, Maddux TM, Tollefson MB, Bond BR, Macinnes A, Yu Y.
Bioorg Med Chem Lett (2009) 19 : 4088 -4091
PubMed 19540112 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.73 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL538896 1 8.22
CHEMBL556514 1 8.00
CHEMBL556863 1 7.94
CHEMBL560408 1 7.60
CHEMBL560687 1 7.50
CHEMBL563130 1 7.47
CHEMBL558338 1 7.44
CHEMBL550817 1 7.38
CHEMBL561952 1 7.14
CHEMBL560609 1 6.95
CHEMBL557755 1 6.94
CHEMBL557266 1 6.82
CHEMBL550007 1 6.71
CHEMBL559889 1 6.62
CHEMBL564374 1 6.50
CHEMBL558729 1 6.46
CHEMBL560545 1 6.43
CHEMBL557467 1 6.34
CHEMBL563661 1 6.06
CHEMBL557059 1 6.04
CHEMBL562208 1 6.04
CHEMBL550131 1 6.01
CHEMBL551948 1 5.94
CHEMBL561088 1 5.93
CHEMBL563669 1 5.92
CHEMBL561548 1 5.73
CHEMBL552025 1 5.70
CHEMBL563637 1 -
CHEMBL558466 1 -
CHEMBL562756 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL538896 IC50 = 6.0 nM 8.22
CHEMBL556514 IC50 = 10.1 nM 8.00
CHEMBL556863 IC50 = 11.6 nM 7.94
CHEMBL560408 IC50 = 25.2 nM 7.60
CHEMBL560687 IC50 = 32.0 nM 7.50
CHEMBL563130 IC50 = 33.5 nM 7.47
CHEMBL558338 IC50 = 36.3 nM 7.44
CHEMBL550817 IC50 = 41.6 nM 7.38
CHEMBL561952 IC50 = 72.0 nM 7.14
CHEMBL560609 IC50 = 112.0 nM 6.95
CHEMBL557755 IC50 = 114.0 nM 6.94
CHEMBL557266 IC50 = 150.0 nM 6.82
CHEMBL550007 IC50 = 195.0 nM 6.71
CHEMBL559889 IC50 = 240.0 nM 6.62
CHEMBL564374 IC50 = 317.0 nM 6.50
CHEMBL558729 IC50 = 350.0 nM 6.46
CHEMBL560545 IC50 = 375.0 nM 6.43
CHEMBL557467 IC50 = 459.0 nM 6.34
CHEMBL563661 IC50 = 871.0 nM 6.06
CHEMBL557059 IC50 = 910.0 nM 6.04
CHEMBL562208 IC50 = 920.0 nM 6.04
CHEMBL550131 IC50 = 979.0 nM 6.01
CHEMBL551948 IC50 = 1160.0 nM 5.94
CHEMBL561088 IC50 = 1170.0 nM 5.93
CHEMBL563669 IC50 = 1190.0 nM 5.92
CHEMBL561548 IC50 = 1850.0 nM 5.73
CHEMBL552025 IC50 = 1980.0 nM 5.70
CHEMBL563637 IC50 > 2000.0 nM -
CHEMBL558466 IC50 > 2000.0 nM -
CHEMBL562756 IC50 > 2000.0 nM -
CHEMBL550478 IC50 - -
CHEMBL565116 IC50 - -
CHEMBL565024 IC50 - -