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Assay Detail

CHEMBL761548

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

Binding
Inhibitory activity against cGMP inhibited Phosphodiesterase 3, isolated from guinea pig ventricular tissue
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Phosphodiesterase 3 (CHEMBL2094125)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Design, synthesis, and biological activities of new thieno[3,2-d] pyrimidines as selective type 4 phosphodiesterase inhibitors.
Crespo MI, Pagès L, Vega A, Segarra V, López M, Doménech T, Miralpeix M, Beleta J, Ryder H, Palacios JM.
J Med Chem (1998) 41 : 4021 -4035
PubMed 9767640 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 4.67 6.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL189 MILRINONE 4.0 1 6.14
CHEMBL281244 1 5.46
CHEMBL30941 1 5.30
CHEMBL414613 1 5.29
CHEMBL31715 1 5.22
CHEMBL128691 1 5.07
CHEMBL30619 1 4.85
CHEMBL288547 1 4.75
CHEMBL28562 1 4.70
CHEMBL30406 1 4.54
CHEMBL30671 1 4.52
CHEMBL434590 1 4.41
CHEMBL30733 1 4.38
CHEMBL422437 1 4.37
CHEMBL31743 1 4.36
CHEMBL335843 1 4.35
CHEMBL128461 1 4.24
CHEMBL132107 1 4.24
CHEMBL30407 1 4.19
CHEMBL31877 1 4.17
CHEMBL31063 1 4.17
CHEMBL30379 1 4.01
CHEMBL132346 1 -
CHEMBL128788 1 -
CHEMBL31795 1 -
CHEMBL31530 1 -
CHEMBL63 ROLIPRAM 2.0 1 -
CHEMBL31439 1 -
CHEMBL341519 1 -
CHEMBL334988 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL189 MILRINONE IC50 = 730.0 nM 6.14
CHEMBL281244 IC50 = 3500.0 nM 5.46
CHEMBL30941 IC50 = 5000.0 nM 5.30
CHEMBL414613 IC50 = 5100.0 nM 5.29
CHEMBL31715 IC50 = 6000.0 nM 5.22
CHEMBL128691 IC50 = 8500.0 nM 5.07
CHEMBL30619 IC50 = 14000.0 nM 4.85
CHEMBL288547 IC50 = 18000.0 nM 4.75
CHEMBL28562 IC50 = 20000.0 nM 4.70
CHEMBL30406 IC50 = 29000.0 nM 4.54
CHEMBL30671 IC50 = 30000.0 nM 4.52
CHEMBL434590 IC50 = 39000.0 nM 4.41
CHEMBL30733 IC50 = 42000.0 nM 4.38
CHEMBL422437 IC50 = 43000.0 nM 4.37
CHEMBL31743 IC50 = 44000.0 nM 4.36
CHEMBL335843 IC50 = 45000.0 nM 4.35
CHEMBL128461 IC50 = 58000.0 nM 4.24
CHEMBL132107 IC50 = 58000.0 nM 4.24
CHEMBL30407 IC50 = 64000.0 nM 4.19
CHEMBL31877 IC50 = 68000.0 nM 4.17
CHEMBL31063 IC50 = 68000.0 nM 4.17
CHEMBL30379 IC50 = 97000.0 nM 4.01
CHEMBL30966 IC50 > 200000.0 nM -
CHEMBL130514 IC50 > 200000.0 nM -
CHEMBL434822 IC50 > 200000.0 nM -
CHEMBL132267 IC50 = 200000.0 nM -
CHEMBL128146 IC50 > 200000.0 nM -
CHEMBL288545 IC50 > 200000.0 nM -
CHEMBL31773 IC50 > 200000.0 nM -
CHEMBL131059 IC50 > 200000.0 nM -
CHEMBL132273 IC50 > 200000.0 nM -
CHEMBL132156 IC50 > 200000.0 nM -
CHEMBL435363 IC50 > 200000.0 nM -
CHEMBL132346 IC50 > 200000.0 nM -
CHEMBL32673 IC50 > 200000.0 nM -
CHEMBL31305 IC50 > 200000.0 nM -
CHEMBL334988 IC50 > 200000.0 nM -
CHEMBL341519 IC50 > 200000.0 nM -
CHEMBL31439 IC50 > 200000.0 nM -
CHEMBL63 ROLIPRAM IC50 = 242000.0 nM -
CHEMBL31530 IC50 > 200000.0 nM -
CHEMBL31795 IC50 > 200000.0 nM -
CHEMBL128788 IC50 > 200000.0 nM -