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Assay Detail

CHEMBL1107382

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

Binding
Inhibition of human recombinant PDE5 after 1.5 hrs by fluorescent polarization assay
31
Total Activities
31
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

cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, molecular modeling and biological evaluation of novel tadalafil analogues as phosphodiesterase 5 and colon tumor cell growth inhibitors, new stereochemical perspective.
Abadi AH, Gary BD, Tinsley HN, Piazza GA, Abdel-Halim M.
Eur J Med Chem (2010) 45 : 1278 -1286
PubMed 20206015 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 5.99 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL779 TADALAFIL 4.0 1 8.40
CHEMBL1099245 1 7.42
CHEMBL1094263 1 7.40
CHEMBL1094590 1 7.30
CHEMBL1097923 1 7.30
CHEMBL1097587 1 7.22
CHEMBL1097584 1 7.00
CHEMBL1096598 1 6.58
CHEMBL1098905 1 6.54
CHEMBL1094268 1 6.50
CHEMBL1099244 1 6.19
CHEMBL1097586 1 5.55
CHEMBL1095632 1 5.51
CHEMBL1094591 1 5.47
CHEMBL1099243 1 5.40
CHEMBL1098959 1 5.25
CHEMBL1097215 1 5.21
CHEMBL1097216 1 4.54
CHEMBL1094589 1 4.50
CHEMBL1094588 1 4.39
CHEMBL1095583 1 4.13
CHEMBL1097585 1 4.06
CHEMBL1099246 1 -
CHEMBL1097921 1 -
CHEMBL1097922 1 -
CHEMBL1097218 1 -
CHEMBL1097217 1 -
CHEMBL1095921 1 -
CHEMBL1094262 1 -
CHEMBL1095631 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL779 TADALAFIL IC50 = 4.0 nM 8.40
CHEMBL1099245 IC50 = 38.0 nM 7.42
CHEMBL1094263 IC50 = 40.0 nM 7.40
CHEMBL1094590 IC50 = 50.0 nM 7.30
CHEMBL1097923 IC50 = 50.0 nM 7.30
CHEMBL1097587 IC50 = 60.0 nM 7.22
CHEMBL1097584 IC50 = 100.0 nM 7.00
CHEMBL1096598 IC50 = 260.0 nM 6.58
CHEMBL1098905 IC50 = 290.0 nM 6.54
CHEMBL1094268 IC50 = 320.0 nM 6.50
CHEMBL1099244 IC50 = 640.0 nM 6.19
CHEMBL1097586 IC50 = 2800.0 nM 5.55
CHEMBL1095632 IC50 = 3100.0 nM 5.51
CHEMBL1094591 IC50 = 3400.0 nM 5.47
CHEMBL1099243 IC50 = 4000.0 nM 5.40
CHEMBL1098959 IC50 = 5600.0 nM 5.25
CHEMBL1097215 IC50 = 6100.0 nM 5.21
CHEMBL1097216 IC50 = 29000.0 nM 4.54
CHEMBL1094589 IC50 = 32000.0 nM 4.50
CHEMBL1094588 IC50 = 41000.0 nM 4.39
CHEMBL1095583 IC50 = 74000.0 nM 4.13
CHEMBL1097585 IC50 = 88000.0 nM 4.06
CHEMBL1099246 IC50 - -
CHEMBL1097921 IC50 - -
CHEMBL1097922 IC50 - -
CHEMBL1097218 IC50 - -
CHEMBL1097217 IC50 - -
CHEMBL1095921 IC50 - -
CHEMBL1094262 IC50 - -
CHEMBL1095631 IC50 - -
CHEMBL1098960 IC50 - -