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Assay Detail

CHEMBL2175239

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Functional
Inhibition of ADP-stimulated platelet aggregation in human platelet rich plasma by light transmission aggregometry based Born method
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Plasma
Cell Type Platelet
Confidence 1 — Organism
Curated By Autocuration

Target

Platelet (CHEMBL4296519)
Type CELL-LINE

Publication

Identification of high-affinity P2Y₁₂ antagonists based on a phenylpyrazole glutamic acid piperazine backbone.
Zech G, Hessler G, Evers A, Weiss T, Florian P, Just M, Czech J, Czechtizky W, Görlitzer J, Ruf S, Kohlmann M, Nazaré M.
J Med Chem (2012) 55 : 8615 -8629
PubMed 22984835 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.97 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2172272 1 8.05
CHEMBL2172149 1 7.89
CHEMBL2172151 1 7.68
CHEMBL2172148 1 7.52
CHEMBL2172273 1 7.42
CHEMBL2172150 1 7.38
CHEMBL2172140 1 7.34
CHEMBL2172133 1 7.16
CHEMBL2172128 1 7.16
CHEMBL2172269 1 7.16
CHEMBL2172161 1 7.14
CHEMBL2172156 1 7.14
CHEMBL2172129 1 7.10
CHEMBL2172267 1 7.04
CHEMBL2172139 1 7.00
CHEMBL2172165 1 6.92
CHEMBL2172132 1 6.92
CHEMBL2172279 1 5.61
CHEMBL2172278 1 5.61
CHEMBL2172280 1 5.60
CHEMBL2172277 1 5.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2172272 IC50 = 9.0 nM 8.05
CHEMBL2172149 IC50 = 13.0 nM 7.89
CHEMBL2172151 IC50 = 21.0 nM 7.68
CHEMBL2172148 IC50 = 30.0 nM 7.52
CHEMBL2172273 IC50 = 38.0 nM 7.42
CHEMBL2172150 IC50 = 42.0 nM 7.38
CHEMBL2172140 IC50 = 46.0 nM 7.34
CHEMBL2172133 IC50 = 70.0 nM 7.16
CHEMBL2172128 IC50 = 69.0 nM 7.16
CHEMBL2172269 IC50 = 70.0 nM 7.16
CHEMBL2172161 IC50 = 73.0 nM 7.14
CHEMBL2172156 IC50 = 72.0 nM 7.14
CHEMBL2172129 IC50 = 79.0 nM 7.10
CHEMBL2172267 IC50 = 91.0 nM 7.04
CHEMBL2172139 IC50 = 100.0 nM 7.00
CHEMBL2172165 IC50 = 120.0 nM 6.92
CHEMBL2172132 IC50 = 120.0 nM 6.92
CHEMBL2172279 IC50 = 2460.0 nM 5.61
CHEMBL2172278 IC50 = 2480.0 nM 5.61
CHEMBL2172280 IC50 = 2510.0 nM 5.60
CHEMBL2172277 IC50 = 2930.0 nM 5.53