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Assay Detail

CHEMBL3367079

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Binding
Antagonist activity at P2Y12 receptor in Sprague-Dawley rat platelet rich plasma assessed as inhibition of ADP-induced aggregation
ChEMBL ↗
91
Total Activities
89
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Plasma
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

P2Y purinoceptor 12 (CHEMBL2188) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

N-[6-(4-butanoyl-5-methyl-1H-pyrazol-1-yl)pyridazin-3-yl]-5-chloro-1-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1H-indole-3-carboxamide (SAR216471), a novel intravenous and oral, reversible, and directly acting P2Y12 antagonist.
Boldron C, Besse A, Bordes MF, Tissandié S, Yvon X, Gau B, Badorc A, Rousseaux T, Barré G, Meneyrol J, Zech G, Nazare M, Fossey V, Pflieger AM, Bonnet-Lignon S, Millet L, Briot C, Dol F, Hérault JP, Savi P, Lassalle G, Delesque N, Herbert JM, Bono F.
J Med Chem (2014) 57 : 7293 -7316
PubMed 25075638 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 91 6.02 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3325894 — — 1 7.70
CHEMBL3325891 — — 1 7.22
CHEMBL3325893 — — 1 6.82
CHEMBL3325804 — — 1 6.70
CHEMBL3325802 — — 1 6.70
CHEMBL3325660 — — 1 6.52
CHEMBL3325803 — — 1 6.52
CHEMBL3325630 — — 1 6.52
CHEMBL3325790 — — 1 6.52
CHEMBL3325805 — — 3 6.52
CHEMBL3325782 — — 1 6.40
CHEMBL3325792 — — 1 6.40
CHEMBL3325791 — — 1 6.40
CHEMBL3325801 — — 1 6.40
CHEMBL3325896 — — 1 6.40
CHEMBL3325452 — — 1 6.40
CHEMBL3325788 — — 1 6.40
CHEMBL3325659 — — 1 6.40
CHEMBL3325779 — — 1 6.40
CHEMBL3325645 — — 1 6.40
CHEMBL3325666 — — 1 6.40
CHEMBL3325664 — — 1 6.40
CHEMBL3325655 — — 1 6.40
CHEMBL3325631 — — 1 6.30
CHEMBL3325651 — — 1 6.30
CHEMBL3325647 — — 1 6.30
CHEMBL3325789 — — 1 6.30
CHEMBL3325783 — — 1 6.30
CHEMBL3325785 — — 1 6.30
CHEMBL3325786 — — 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3325894 — IC50 = 20.0 nM 7.70
CHEMBL3325891 — IC50 = 60.0 nM 7.22
CHEMBL3325893 — IC50 = 150.0 nM 6.82
CHEMBL3325802 — IC50 = 200.0 nM 6.70
CHEMBL3325804 — IC50 = 200.0 nM 6.70
CHEMBL3325805 — IC50 = 300.0 nM 6.52
CHEMBL3325805 — IC50 = 300.0 nM 6.52
CHEMBL3325660 — IC50 = 300.0 nM 6.52
CHEMBL3325803 — IC50 = 300.0 nM 6.52
CHEMBL3325630 — IC50 = 300.0 nM 6.52
CHEMBL3325790 — IC50 = 300.0 nM 6.52
CHEMBL3325655 — IC50 = 400.0 nM 6.40
CHEMBL3325792 — IC50 = 400.0 nM 6.40
CHEMBL3325805 — IC50 = 400.0 nM 6.40
CHEMBL3325801 — IC50 = 400.0 nM 6.40
CHEMBL3325896 — IC50 = 400.0 nM 6.40
CHEMBL3325791 — IC50 = 400.0 nM 6.40
CHEMBL3325452 — IC50 = 400.0 nM 6.40
CHEMBL3325645 — IC50 = 400.0 nM 6.40
CHEMBL3325788 — IC50 = 400.0 nM 6.40
CHEMBL3325782 — IC50 = 400.0 nM 6.40
CHEMBL3325779 — IC50 = 400.0 nM 6.40
CHEMBL3325666 — IC50 = 400.0 nM 6.40
CHEMBL3325659 — IC50 = 400.0 nM 6.40
CHEMBL3325664 — IC50 = 400.0 nM 6.40
CHEMBL3325786 — IC50 = 500.0 nM 6.30
CHEMBL3325789 — IC50 = 500.0 nM 6.30
CHEMBL3325647 — IC50 = 500.0 nM 6.30
CHEMBL3325785 — IC50 = 500.0 nM 6.30
CHEMBL3325651 — IC50 = 500.0 nM 6.30
CHEMBL3325631 — IC50 = 500.0 nM 6.30
CHEMBL3325783 — IC50 = 500.0 nM 6.30
CHEMBL3325793 — IC50 = 600.0 nM 6.22
CHEMBL3325806 — IC50 = 600.0 nM 6.22
CHEMBL3325643 — IC50 = 600.0 nM 6.22
CHEMBL3325663 — IC50 = 700.0 nM 6.16
CHEMBL3325807 — IC50 = 700.0 nM 6.16
CHEMBL3325665 — IC50 = 700.0 nM 6.16
CHEMBL3325656 — IC50 = 700.0 nM 6.16
CHEMBL3325632 — IC50 = 800.0 nM 6.10
CHEMBL3325640 — IC50 = 800.0 nM 6.10
CHEMBL3325662 — IC50 = 800.0 nM 6.10
CHEMBL3325644 — IC50 = 800.0 nM 6.10
CHEMBL3325780 — IC50 = 800.0 nM 6.10
CHEMBL3325657 — IC50 = 900.0 nM 6.05
CHEMBL3325658 — IC50 = 900.0 nM 6.05
CHEMBL3325642 — IC50 = 900.0 nM 6.05
CHEMBL3325636 — IC50 = 1000.0 nM 6.00
CHEMBL3325634 — IC50 = 1000.0 nM 6.00
CHEMBL3325639 — IC50 = 1000.0 nM 6.00