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Assay Detail

CHEMBL758014

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

Binding
In vitro inhibition of PDE-V isolated from porcine pulmonary artery.
23
Total Activities
23
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

Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: analogues of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase.
Coates WJ, Connolly B, Dhanak D, Flynn ST, Worby A.
J Med Chem (1993) 36 : 1387 -1392
PubMed 8388468 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.01 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL32183 1 6.00
CHEMBL28871 1 6.00
CHEMBL28079 ZAPRINAST 2.0 1 6.00
CHEMBL542813 1 6.00
CHEMBL280830 1 5.70
CHEMBL286021 1 5.52
CHEMBL27627 1 5.40
CHEMBL28566 1 5.40
CHEMBL417477 1 5.22
CHEMBL28835 1 5.22
CHEMBL286042 1 4.82
CHEMBL31359 1 4.75
CHEMBL286020 SULMAZOLE 2.0 1 4.68
CHEMBL281663 1 4.62
CHEMBL31954 1 4.62
CHEMBL32093 1 4.58
CHEMBL432659 1 4.48
CHEMBL543042 1 4.47
CHEMBL28597 1 4.43
CHEMBL28240 1 4.40
CHEMBL553515 1 4.38
CHEMBL2110680 ISOMAZOLE 2.0 1 4.24
CHEMBL31964 1 4.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL32183 IC50 = 1000.0 nM 6.00
CHEMBL28871 IC50 = 1000.0 nM 6.00
CHEMBL28079 ZAPRINAST IC50 = 1000.0 nM 6.00
CHEMBL542813 IC50 = 1000.0 nM 6.00
CHEMBL280830 IC50 = 2000.0 nM 5.70
CHEMBL286021 IC50 = 3000.0 nM 5.52
CHEMBL27627 IC50 = 4000.0 nM 5.40
CHEMBL28566 IC50 = 4000.0 nM 5.40
CHEMBL417477 IC50 = 6000.0 nM 5.22
CHEMBL28835 IC50 = 6000.0 nM 5.22
CHEMBL286042 IC50 = 15000.0 nM 4.82
CHEMBL31359 IC50 = 18000.0 nM 4.75
CHEMBL286020 SULMAZOLE IC50 = 21000.0 nM 4.68
CHEMBL281663 IC50 = 24000.0 nM 4.62
CHEMBL31954 IC50 = 24000.0 nM 4.62
CHEMBL32093 IC50 = 26000.0 nM 4.58
CHEMBL432659 IC50 = 33000.0 nM 4.48
CHEMBL543042 IC50 = 34000.0 nM 4.47
CHEMBL28597 IC50 = 37000.0 nM 4.43
CHEMBL28240 IC50 = 40000.0 nM 4.40
CHEMBL553515 IC50 = 42000.0 nM 4.38
CHEMBL2110680 ISOMAZOLE IC50 = 58000.0 nM 4.24
CHEMBL31964 IC50 = 64000.0 nM 4.19