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Assay Detail

CHEMBL696421

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

Functional
Inhibition of platelet aggregation using adenosine diphosphate (ADP) as activating agent in human platelet rich plasma (PRP)
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Plasma
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

P2Y purinoceptor 12 (CHEMBL2001)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibitors of blood platelet cAMP phosphodiesterase. 2. Structure-activity relationships associated with 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones substituted with functionalized side chains.
Meanwell NA, Pearce BC, Roth HR, Smith EC, Wedding DL, Wright JJ, Buchanan JO, Baryla UM, Gamberdella M, Gillespie E.
J Med Chem (1992) 35 : 2672 -2687
PubMed 1321910 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 44 6.38 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL90804 1 9.15
CHEMBL90237 1 9.00
CHEMBL431799 1 9.00
CHEMBL90195 1 8.40
CHEMBL91368 1 8.15
CHEMBL88245 1 8.00
CHEMBL90881 1 7.92
CHEMBL93688 1 7.80
CHEMBL92264 1 7.70
CHEMBL88583 1 7.70
CHEMBL423864 1 7.42
CHEMBL88444 1 7.10
CHEMBL91478 1 7.05
CHEMBL328149 1 7.05
CHEMBL91359 1 7.00
CHEMBL90414 1 6.89
CHEMBL90958 1 6.72
CHEMBL69139 LIXAZINONE 2.0 1 6.36
CHEMBL88764 1 6.27
CHEMBL91527 1 6.27
CHEMBL92269 1 6.22
CHEMBL88708 1 5.96
CHEMBL91422 1 5.91
CHEMBL420980 1 5.52
CHEMBL330280 1 5.52
CHEMBL88799 1 5.28
CHEMBL91356 1 5.11
CHEMBL88108 1 5.02
CHEMBL314763 1 4.93
CHEMBL313463 1 4.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL90804 EC50 = 0.7 nM 9.15
CHEMBL90237 EC50 = 1.0 nM 9.00
CHEMBL431799 EC50 = 1.0 nM 9.00
CHEMBL90195 EC50 = 4.0 nM 8.40
CHEMBL91368 EC50 = 7.0 nM 8.15
CHEMBL88245 EC50 = 10.0 nM 8.00
CHEMBL90881 EC50 = 12.0 nM 7.92
CHEMBL93688 EC50 = 16.0 nM 7.80
CHEMBL92264 EC50 = 20.0 nM 7.70
CHEMBL88583 EC50 = 20.0 nM 7.70
CHEMBL423864 EC50 = 38.0 nM 7.42
CHEMBL88444 EC50 = 80.0 nM 7.10
CHEMBL91478 EC50 = 90.0 nM 7.05
CHEMBL328149 EC50 = 90.0 nM 7.05
CHEMBL91359 EC50 = 100.0 nM 7.00
CHEMBL90414 EC50 = 130.0 nM 6.89
CHEMBL90958 EC50 = 190.0 nM 6.72
CHEMBL69139 LIXAZINONE EC50 = 440.0 nM 6.36
CHEMBL88764 EC50 = 540.0 nM 6.27
CHEMBL91527 EC50 = 540.0 nM 6.27
CHEMBL92269 EC50 = 600.0 nM 6.22
CHEMBL88708 EC50 = 1100.0 nM 5.96
CHEMBL91422 EC50 = 1220.0 nM 5.91
CHEMBL330280 EC50 = 3020.0 nM 5.52
CHEMBL420980 EC50 = 3000.0 nM 5.52
CHEMBL88799 EC50 = 5260.0 nM 5.28
CHEMBL91356 EC50 = 7840.0 nM 5.11
CHEMBL88108 EC50 = 9600.0 nM 5.02
CHEMBL314763 EC50 = 11870.0 nM 4.93
CHEMBL313463 EC50 = 14970.0 nM 4.83
CHEMBL91204 EC50 = 15520.0 nM 4.81
CHEMBL88877 EC50 = 29850.0 nM 4.53
CHEMBL420618 EC50 = 33000.0 nM 4.48
CHEMBL91570 EC50 = 45280.0 nM 4.34
CHEMBL88707 EC50 = 49500.0 nM 4.30
CHEMBL90120 EC50 = 51000.0 nM 4.29
CHEMBL90168 EC50 = 71600.0 nM 4.14
CHEMBL88835 EC50 > 100000.0 nM -
CHEMBL760 ANAGRELIDE EC50 = 1.05 PuM -
CHEMBL91579 EC50 > 100000.0 nM -
CHEMBL327580 EC50 > 26500.0 nM -
CHEMBL313609 EC50 > 100000.0 nM -
CHEMBL88265 EC50 > 112000.0 nM -
CHEMBL91224 EC50 > 106000.0 nM -