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Assay Detail

CHEMBL3367077

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

Binding
Displacement of [33P]2MeS-ADP from P2Y12 receptor (unknown origin) transfected in CHO cells after 30 mins by scintillation counting analysis
ChEMBL ↗
91
Total Activities
89
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

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 7.25 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3326907 — — 1 9.05
CHEMBL3325627 — — 1 8.29
CHEMBL3325894 — — 1 8.15
CHEMBL3326906 — — 1 8.15
CHEMBL3325805 — — 3 8.15
CHEMBL3325802 — — 1 7.96
CHEMBL3325803 — — 1 7.96
CHEMBL3325804 — — 1 7.96
CHEMBL3325788 — — 1 7.92
CHEMBL3325785 — — 1 7.82
CHEMBL3325801 — — 1 7.82
CHEMBL3325891 — — 1 7.77
CHEMBL3326903 — — 1 7.77
CHEMBL3325782 — — 1 7.72
CHEMBL3325783 — — 1 7.72
CHEMBL3325660 — — 1 7.70
CHEMBL3325789 — — 1 7.66
CHEMBL3326905 — — 1 7.62
CHEMBL3325781 — — 1 7.58
CHEMBL3325666 — — 1 7.57
CHEMBL3325452 — — 1 7.57
CHEMBL3325780 — — 1 7.55
CHEMBL3325661 — — 1 7.54
CHEMBL3325629 — — 1 7.51
CHEMBL3325631 — — 1 7.51
CHEMBL3325656 — — 1 7.48
CHEMBL3325793 — — 1 7.47
CHEMBL3325630 — — 1 7.41
CHEMBL3325893 — — 1 7.40
CHEMBL3325659 — — 1 7.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3326907 — IC50 = 0.9 nM 9.05
CHEMBL3325627 — IC50 = 5.1 nM 8.29
CHEMBL3326906 — IC50 = 7.0 nM 8.15
CHEMBL3325805 — IC50 = 7.0 nM 8.15
CHEMBL3325894 — IC50 = 7.0 nM 8.15
CHEMBL3325805 — IC50 = 8.0 nM 8.10
CHEMBL3325802 — IC50 = 11.0 nM 7.96
CHEMBL3325803 — IC50 = 11.0 nM 7.96
CHEMBL3325804 — IC50 = 11.0 nM 7.96
CHEMBL3325788 — IC50 = 12.0 nM 7.92
CHEMBL3325805 — IC50 = 12.0 nM 7.92
CHEMBL3325785 — IC50 = 15.0 nM 7.82
CHEMBL3325801 — IC50 = 15.0 nM 7.82
CHEMBL3326903 — IC50 = 17.0 nM 7.77
CHEMBL3325891 — IC50 = 17.0 nM 7.77
CHEMBL3325782 — IC50 = 19.0 nM 7.72
CHEMBL3325783 — IC50 = 19.0 nM 7.72
CHEMBL3325660 — IC50 = 20.0 nM 7.70
CHEMBL3325789 — IC50 = 22.0 nM 7.66
CHEMBL3326905 — IC50 = 24.0 nM 7.62
CHEMBL3325781 — IC50 = 26.0 nM 7.58
CHEMBL3325666 — IC50 = 27.0 nM 7.57
CHEMBL3325452 — IC50 = 27.0 nM 7.57
CHEMBL3325780 — IC50 = 28.0 nM 7.55
CHEMBL3325661 — IC50 = 29.0 nM 7.54
CHEMBL3325629 — IC50 = 31.0 nM 7.51
CHEMBL3325631 — IC50 = 31.0 nM 7.51
CHEMBL3325656 — IC50 = 33.0 nM 7.48
CHEMBL3325793 — IC50 = 34.0 nM 7.47
CHEMBL3325630 — IC50 = 39.0 nM 7.41
CHEMBL3325893 — IC50 = 40.0 nM 7.40
CHEMBL3325659 — IC50 = 41.0 nM 7.39
CHEMBL3325662 — IC50 = 44.0 nM 7.36
CHEMBL3325648 — IC50 = 46.0 nM 7.34
CHEMBL3325665 — IC50 = 46.0 nM 7.34
CHEMBL3325640 — IC50 = 47.0 nM 7.33
CHEMBL3326904 — IC50 = 47.0 nM 7.33
CHEMBL3325791 — IC50 = 48.0 nM 7.32
CHEMBL3325896 — IC50 = 48.0 nM 7.32
CHEMBL3325790 — IC50 = 48.0 nM 7.32
CHEMBL3325792 — IC50 = 50.0 nM 7.30
CHEMBL3325632 — IC50 = 61.0 nM 7.21
CHEMBL3325637 — IC50 = 61.0 nM 7.21
CHEMBL3325649 — IC50 = 65.0 nM 7.19
CHEMBL3325657 — IC50 = 66.0 nM 7.18
CHEMBL3325784 — IC50 = 66.0 nM 7.18
CHEMBL3325787 — IC50 = 70.0 nM 7.16
CHEMBL3325641 — IC50 = 71.0 nM 7.15
CHEMBL3325644 — IC50 = 71.0 nM 7.15
CHEMBL3325650 — IC50 = 73.0 nM 7.14