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Assay Detail

CHEMBL2415776

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

Binding
Inhibition of PDE5 (unknown origin)
18
Total Activities
18
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

Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5.
Gong X, Wang G, Ren J, Liu Z, Wang Z, Chen T, Yang X, Jiang X, Shen J, Jiang H, Aisa HA, Xu Y, Li J.
Bioorg Med Chem Lett (2013) 23 : 4944 -4947
PubMed 23867165 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.82 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2414316 1 8.77
CHEMBL2414311 1 8.55
CHEMBL2414317 1 8.40
CHEMBL2414312 1 8.35
CHEMBL2414308 1 8.21
CHEMBL2414315 1 8.06
CHEMBL2414313 1 8.02
CHEMBL2414303 1 7.99
CHEMBL2414310 1 7.96
CHEMBL2414319 1 7.76
CHEMBL2414314 1 7.74
CHEMBL2414318 1 7.67
CHEMBL2414307 1 7.59
CHEMBL2414309 1 7.53
CHEMBL2414302 1 7.32
CHEMBL2414305 1 7.13
CHEMBL2414304 1 7.11
CHEMBL2414306 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2414316 IC50 = 1.7 nM 8.77
CHEMBL2414311 IC50 = 2.8 nM 8.55
CHEMBL2414317 IC50 = 4.0 nM 8.40
CHEMBL2414312 IC50 = 4.5 nM 8.35
CHEMBL2414308 IC50 = 6.2 nM 8.21
CHEMBL2414315 IC50 = 8.8 nM 8.06
CHEMBL2414313 IC50 = 9.6 nM 8.02
CHEMBL2414303 IC50 = 10.2 nM 7.99
CHEMBL2414310 IC50 = 11.1 nM 7.96
CHEMBL2414319 IC50 = 17.4 nM 7.76
CHEMBL2414314 IC50 = 18.2 nM 7.74
CHEMBL2414318 IC50 = 21.3 nM 7.67
CHEMBL2414307 IC50 = 25.5 nM 7.59
CHEMBL2414309 IC50 = 29.3 nM 7.53
CHEMBL2414302 IC50 = 48.0 nM 7.32
CHEMBL2414305 IC50 = 74.0 nM 7.13
CHEMBL2414304 IC50 = 77.0 nM 7.11
CHEMBL2414306 IC50 = 272.0 nM 6.57