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Assay Detail

CHEMBL761832

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Binding
Evaluated for inhibitory activity against Phosphodiesterase 5 (PDE5) purified from bovine lung
ChEMBL ↗
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL3478) ↗
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Potent tetracyclic guanine inhibitors of PDE1 and PDE5 cyclic guanosine monophosphate phosphodiesterases with oral antihypertensive activity.
Ahn HS, Bercovici A, Boykow G, Bronnenkant A, Chackalamannil S, Chow J, Cleven R, Cook J, Czarniecki M, Domalski C, Fawzi A, Green M, Gündes A, Ho G, Laudicina M, Lindo N, Ma K, Manna M, McKittrick B, Mirzai B, Nechuta T, Neustadt B, Puchalski C, Pula K, Zhang H.
J Med Chem (1997) 40 : 2196 -2210
PubMed 9216839 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 6.39 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70569 — — 1 8.40
CHEMBL305618 — — 1 8.40
CHEMBL18745 — — 1 8.00
CHEMBL304161 — — 1 7.96
CHEMBL72812 — — 1 7.72
CHEMBL446663 — — 1 7.72
CHEMBL308828 — — 1 7.72
CHEMBL305617 — — 1 7.58
CHEMBL305988 — — 1 7.47
CHEMBL303154 — — 1 7.37
CHEMBL18744 — — 1 7.30
CHEMBL304389 — — 1 7.18
CHEMBL68152 — — 1 7.10
CHEMBL431772 — — 1 7.00
CHEMBL306666 — — 1 6.96
CHEMBL71204 — — 1 6.92
CHEMBL305989 — — 1 6.92
CHEMBL305237 — — 1 6.75
CHEMBL431377 — — 1 6.70
CHEMBL307640 — — 1 6.70
CHEMBL71768 — — 1 6.65
CHEMBL419447 — — 1 6.62
CHEMBL430802 — — 1 6.56
CHEMBL308249 — — 1 6.52
CHEMBL70837 — — 1 6.40
CHEMBL70471 — — 1 6.38
CHEMBL28079 ZAPRINAST 2.0 1 6.30
CHEMBL307379 — — 1 6.29
CHEMBL409425 — — 1 6.25
CHEMBL303917 — — 1 6.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70569 — IC50 = 4.0 nM 8.40
CHEMBL305618 — IC50 = 4.0 nM 8.40
CHEMBL18745 — IC50 = 10.0 nM 8.00
CHEMBL304161 — IC50 = 11.0 nM 7.96
CHEMBL72812 — IC50 = 19.0 nM 7.72
CHEMBL446663 — IC50 = 19.0 nM 7.72
CHEMBL308828 — IC50 = 19.0 nM 7.72
CHEMBL305617 — IC50 = 26.0 nM 7.58
CHEMBL305988 — IC50 = 34.0 nM 7.47
CHEMBL303154 — IC50 = 43.0 nM 7.37
CHEMBL18744 — IC50 = 50.0 nM 7.30
CHEMBL304389 — IC50 = 66.0 nM 7.18
CHEMBL68152 — IC50 = 80.0 nM 7.10
CHEMBL431772 — IC50 = 100.0 nM 7.00
CHEMBL306666 — IC50 = 110.0 nM 6.96
CHEMBL71204 — IC50 = 120.0 nM 6.92
CHEMBL305989 — IC50 = 120.0 nM 6.92
CHEMBL305237 — IC50 = 180.0 nM 6.75
CHEMBL431377 — IC50 = 200.0 nM 6.70
CHEMBL307640 — IC50 = 200.0 nM 6.70
CHEMBL71768 — IC50 = 225.0 nM 6.65
CHEMBL419447 — IC50 = 240.0 nM 6.62
CHEMBL430802 — IC50 = 275.0 nM 6.56
CHEMBL308249 — IC50 = 305.0 nM 6.52
CHEMBL70837 — IC50 = 400.0 nM 6.40
CHEMBL70471 — IC50 = 420.0 nM 6.38
CHEMBL28079 ZAPRINAST IC50 = 500.0 nM 6.30
CHEMBL307379 — IC50 = 510.0 nM 6.29
CHEMBL409425 — IC50 = 560.0 nM 6.25
CHEMBL303917 — IC50 = 590.0 nM 6.23
CHEMBL70295 — IC50 = 610.0 nM 6.21
CHEMBL303385 — IC50 = 800.0 nM 6.10
CHEMBL275204 — IC50 = 800.0 nM 6.10
CHEMBL308199 — IC50 = 1000.0 nM 6.00
CHEMBL306426 — IC50 = 1200.0 nM 5.92
CHEMBL71874 — IC50 = 1500.0 nM 5.82
CHEMBL278644 — IC50 = 2400.0 nM 5.62
CHEMBL307232 — IC50 = 2900.0 nM 5.54
CHEMBL422235 — IC50 = 3300.0 nM 5.48
CHEMBL303010 — IC50 = 4000.0 nM 5.40
CHEMBL71824 — IC50 = 4300.0 nM 5.37
CHEMBL68706 — IC50 = 4500.0 nM 5.35
CHEMBL69324 — IC50 = 5600.0 nM 5.25
CHEMBL303920 — IC50 = 6000.0 nM 5.22
CHEMBL303671 — IC50 = 6200.0 nM 5.21
CHEMBL308973 — IC50 = 7500.0 nM 5.12
CHEMBL306417 — IC50 = 10000.0 nM 5.00
CHEMBL307639 — IC50 = 10000.0 nM 5.00
CHEMBL71300 — IC50 = 13000.0 nM 4.89
CHEMBL308747 — IC50 = 16000.0 nM 4.80