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Assay Detail

CHEMBL768652

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Functional
Inhibition of human platelet aggregation cAMP PDE in vitro
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 3 (CHEMBL2094125)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Inhibitors of blood platelet cAMP phosphodiesterase. 4. Structural variation of the side-chain terminus of water-soluble 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives.
Meanwell NA, Hewawasam P, Thomas JA, Wright JJ, Russell JW, Gamberdella M, Goldenberg HJ, Seiler SM, Zavoico GB.
J Med Chem (1993) 36 : 3251 -3264
PubMed 8230115 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.81 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1203032 1 9.20
CHEMBL1203039 1 9.09
CHEMBL1203053 1 9.09
CHEMBL1203031 1 9.08
CHEMBL1203034 1 8.99
CHEMBL1203083 1 8.96
CHEMBL1203086 1 8.95
CHEMBL1203024 1 8.95
CHEMBL1203019 1 8.95
CHEMBL1203063 1 8.90
CHEMBL1203069 1 8.59
CHEMBL1203057 1 8.56
CHEMBL1203091 1 8.30
CHEMBL1203068 1 8.29
CHEMBL1203092 1 8.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1203032 IC50 = 0.63 nM 9.20
CHEMBL1203039 IC50 = 0.81 nM 9.09
CHEMBL1203053 IC50 = 0.81 nM 9.09
CHEMBL1203031 IC50 = 0.84 nM 9.08
CHEMBL1203034 IC50 = 1.03 nM 8.99
CHEMBL1203083 IC50 = 1.11 nM 8.96
CHEMBL1203086 IC50 = 1.13 nM 8.95
CHEMBL1203024 IC50 = 1.13 nM 8.95
CHEMBL1203019 IC50 = 1.13 nM 8.95
CHEMBL1203063 IC50 = 1.25 nM 8.90
CHEMBL1203069 IC50 = 2.56 nM 8.59
CHEMBL1203057 IC50 = 2.78 nM 8.56
CHEMBL1203091 IC50 = 4.96 nM 8.30
CHEMBL1203068 IC50 = 5.14 nM 8.29
CHEMBL1203092 IC50 = 5.42 nM 8.27