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Assay Detail

CHEMBL762502

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

Binding
50% inhibitory concentration against phosphodiesterase 5 (PDE5) from porcine platelets
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.
Watanabe N, Adachi H, Takase Y, Ozaki H, Matsukura M, Miyazaki K, Ishibashi K, Ishihara H, Kodama K, Nishino M, Kakiki M, Kabasawa Y.
J Med Chem (2000) 43 : 2523 -2529
PubMed 10891111 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 8.50 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL542166 1 9.52
CHEMBL545472 1 9.49
CHEMBL544305 1 9.30
CHEMBL553075 1 9.28
CHEMBL553960 1 9.26
CHEMBL542418 1 9.15
CHEMBL545715 1 9.15
CHEMBL545012 1 9.15
CHEMBL545243 1 9.14
CHEMBL542663 1 9.10
CHEMBL557200 1 9.07
CHEMBL553348 1 9.03
CHEMBL555168 1 9.02
CHEMBL543130 1 8.96
CHEMBL544548 1 8.92
CHEMBL554047 1 8.91
CHEMBL545476 1 8.82
CHEMBL540044 1 8.77
CHEMBL553076 1 8.72
CHEMBL541830 1 8.70
CHEMBL1737 SILDENAFIL CITRATE 4.0 1 8.66
CHEMBL556618 1 8.59
CHEMBL544310 1 8.57
CHEMBL545242 1 8.52
CHEMBL554459 1 8.51
CHEMBL25616 1 8.43
CHEMBL539789 1 8.36
CHEMBL552689 1 8.17
CHEMBL544546 1 8.17
CHEMBL558019 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL542166 IC50 = 0.3 nM 9.52
CHEMBL545472 IC50 = 0.32 nM 9.49
CHEMBL544305 IC50 = 0.5 nM 9.30
CHEMBL553075 IC50 = 0.53 nM 9.28
CHEMBL553960 IC50 = 0.55 nM 9.26
CHEMBL542418 IC50 = 0.7 nM 9.15
CHEMBL545715 IC50 = 0.7 nM 9.15
CHEMBL545012 IC50 = 0.7 nM 9.15
CHEMBL545243 IC50 = 0.73 nM 9.14
CHEMBL542663 IC50 = 0.79 nM 9.10
CHEMBL557200 IC50 = 0.86 nM 9.07
CHEMBL553348 IC50 = 0.93 nM 9.03
CHEMBL555168 IC50 = 0.95 nM 9.02
CHEMBL543130 IC50 = 1.1 nM 8.96
CHEMBL544548 IC50 = 1.2 nM 8.92
CHEMBL554047 IC50 = 1.23 nM 8.91
CHEMBL545476 IC50 = 1.5 nM 8.82
CHEMBL540044 IC50 = 1.7 nM 8.77
CHEMBL553076 IC50 = 1.9 nM 8.72
CHEMBL541830 IC50 = 2.0 nM 8.70
CHEMBL1737 SILDENAFIL CITRATE IC50 = 2.2 nM 8.66
CHEMBL556618 IC50 = 2.6 nM 8.59
CHEMBL544310 IC50 = 2.7 nM 8.57
CHEMBL545242 IC50 = 3.0 nM 8.52
CHEMBL554459 IC50 = 3.1 nM 8.51
CHEMBL25616 IC50 = 3.7 nM 8.43
CHEMBL539789 IC50 = 4.4 nM 8.36
CHEMBL552689 IC50 = 6.7 nM 8.17
CHEMBL544546 IC50 = 6.8 nM 8.17
CHEMBL558019 IC50 = 11.0 nM 7.96
CHEMBL3084583 IC50 = 12.0 nM 7.92
CHEMBL544540 IC50 = 14.0 nM 7.85
CHEMBL542899 IC50 = 19.0 nM 7.72
CHEMBL545470 IC50 = 150.0 nM 6.82
CHEMBL552862 IC50 = 600.0 nM 6.22
CHEMBL553934 IC50 = 58000.0 nM 4.24
CHEMBL189 MILRINONE IC50 > 100000.0 nM -
CHEMBL63 ROLIPRAM IC50 > 100000.0 nM -