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Assay Detail

CHEMBL1042744

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Binding
Inhibition of PDE5
ChEMBL ↗
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one.
Hughes RO, Walker JK, Rogier DJ, Heasley SE, Blevis-Bal RM, Benson AG, Jacobsen EJ, Cubbage JW, Fobian YM, Owen DR, Freskos JN, Molyneaux JM, Brown DL, Acker BA, Maddux TM, Tollefson MB, Moon JB, Mischke BV, Rumsey JM, Zheng Y, MacInnes A, Bond BR, Yu Y.
Bioorg Med Chem Lett (2009) 19 : 5209 -5213
PubMed 19631533 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 9.46 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL569481 — — 1 10.40
CHEMBL567470 — — 1 10.30
CHEMBL584270 — — 1 10.30
CHEMBL565305 — — 1 10.22
CHEMBL551052 — — 1 10.15
CHEMBL585918 — — 1 10.15
CHEMBL568839 — — 1 10.15
CHEMBL566598 — — 1 10.10
CHEMBL566367 — — 1 10.05
CHEMBL567471 — — 1 10.00
CHEMBL566797 — — 1 9.96
CHEMBL567445 — — 1 9.89
CHEMBL569264 — — 1 9.89
CHEMBL569492 — — 1 9.85
CHEMBL567016 — — 1 9.85
CHEMBL565306 — — 1 9.82
CHEMBL584317 — — 1 9.77
CHEMBL566375 — — 1 9.62
CHEMBL583854 — — 1 9.60
CHEMBL567469 — — 1 9.60
CHEMBL567447 — — 1 9.59
CHEMBL569045 — — 1 9.55
CHEMBL566820 — — 1 9.49
CHEMBL584285 — — 1 9.49
CHEMBL551250 — — 1 9.47
CHEMBL584056 — — 1 9.47
CHEMBL569491 — — 1 9.44
CHEMBL579669 — — 1 9.42
CHEMBL571912 — — 1 9.37
CHEMBL585015 — — 1 9.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL569481 — IC50 = 0.04 nM 10.40
CHEMBL567470 — IC50 = 0.05 nM 10.30
CHEMBL584270 — IC50 = 0.05 nM 10.30
CHEMBL565305 — IC50 = 0.06 nM 10.22
CHEMBL551052 — IC50 = 0.07 nM 10.15
CHEMBL585918 — IC50 = 0.07 nM 10.15
CHEMBL568839 — IC50 = 0.07 nM 10.15
CHEMBL566598 — IC50 = 0.08 nM 10.10
CHEMBL566367 — IC50 = 0.09 nM 10.05
CHEMBL567471 — IC50 = 0.1 nM 10.00
CHEMBL566797 — IC50 = 0.11 nM 9.96
CHEMBL569264 — IC50 = 0.13 nM 9.89
CHEMBL567445 — IC50 = 0.13 nM 9.89
CHEMBL569492 — IC50 = 0.14 nM 9.85
CHEMBL567016 — IC50 = 0.14 nM 9.85
CHEMBL565306 — IC50 = 0.15 nM 9.82
CHEMBL584317 — IC50 = 0.17 nM 9.77
CHEMBL566375 — IC50 = 0.24 nM 9.62
CHEMBL583854 — IC50 = 0.25 nM 9.60
CHEMBL567469 — IC50 = 0.25 nM 9.60
CHEMBL567447 — IC50 = 0.26 nM 9.59
CHEMBL569045 — IC50 = 0.28 nM 9.55
CHEMBL584285 — IC50 = 0.32 nM 9.49
CHEMBL566820 — IC50 = 0.32 nM 9.49
CHEMBL551250 — IC50 = 0.34 nM 9.47
CHEMBL584056 — IC50 = 0.34 nM 9.47
CHEMBL569491 — IC50 = 0.36 nM 9.44
CHEMBL579669 — IC50 = 0.38 nM 9.42
CHEMBL571912 — IC50 = 0.43 nM 9.37
CHEMBL585015 — IC50 = 0.54 nM 9.27
CHEMBL567446 — IC50 = 0.55 nM 9.26
CHEMBL571693 — IC50 = 0.68 nM 9.17
CHEMBL571469 — IC50 = 0.68 nM 9.17
CHEMBL583835 — IC50 = 0.71 nM 9.15
CHEMBL567229 — IC50 = 0.78 nM 9.11
CHEMBL585352 — IC50 = 0.88 nM 9.06
CHEMBL585327 — IC50 = 0.9 nM 9.05
CHEMBL565308 — IC50 = 1.05 nM 8.98
CHEMBL567252 — IC50 = 1.1 nM 8.96
CHEMBL569265 — IC50 = 1.17 nM 8.93
CHEMBL567255 — IC50 = 1.17 nM 8.93
CHEMBL571913 — IC50 = 1.65 nM 8.78
CHEMBL566819 — IC50 = 2.59 nM 8.59
CHEMBL565331 — IC50 = 2.59 nM 8.59
CHEMBL565518 — IC50 = 2.95 nM 8.53
CHEMBL567251 — IC50 = 4.0 nM 8.40
CHEMBL566596 — IC50 = 16.3 nM 7.79