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Assay Detail

CHEMBL3816044

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

Binding
Agonist activity at mouse P2Y10 receptor expressed in HEK293A cells after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
108
Total Activities
36
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293-A
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Putative P2Y purinoceptor 10 (CHEMBL3562168)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Conformational Constraint of the Glycerol Moiety of Lysophosphatidylserine Affords Compounds with Receptor Subtype Selectivity.
Jung S, Inoue A, Nakamura S, Kishi T, Uwamizu A, Sayama M, Ikubo M, Otani Y, Kano K, Makide K, Aoki J, Ohwada T.
J Med Chem (2016) 59 : 3750 -3776
PubMed 27077565 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 69 6.96 8.18
Emax 36 - -
pEC50 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3814492 3 8.18
CHEMBL3813843 3 7.77
CHEMBL1742484 3 7.61
CHEMBL3813751 3 7.38
CHEMBL3815090 3 7.35
CHEMBL4299634 3 6.54
CHEMBL3814147 3 6.49
CHEMBL4299669 3 6.35
CHEMBL4299658 3 6.35
CHEMBL3814763 3 6.33
CHEMBL3814009 3 6.22
CHEMBL3813950 3 -
CHEMBL3814525 3 -
CHEMBL3815069 3 -
CHEMBL3815141 3 -
CHEMBL3814818 3 -
CHEMBL3813767 3 -
CHEMBL3814440 3 -
CHEMBL3814124 3 -
CHEMBL3814356 3 -
CHEMBL3814527 3 -
CHEMBL3814437 3 -
CHEMBL4299652 3 -
CHEMBL3814235 3 -
CHEMBL3814095 3 -
CHEMBL4299627 3 -
CHEMBL3814707 3 -
CHEMBL3813812 3 -
CHEMBL4299628 3 -
CHEMBL3814643 3 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3814492 EC50 = 6.607 nM 8.18
CHEMBL3814492 EC50 = 6.7 nM 8.17
CHEMBL3813843 EC50 = 17.0 nM 7.77
CHEMBL3813843 EC50 = 16.98 nM 7.77
CHEMBL1742484 EC50 = 24.55 nM 7.61
CHEMBL1742484 EC50 = 25.0 nM 7.60
CHEMBL3813751 EC50 = 41.69 nM 7.38
CHEMBL3813751 EC50 = 42.0 nM 7.38
CHEMBL3815090 EC50 = 44.67 nM 7.35
CHEMBL3815090 EC50 = 45.0 nM 7.35
CHEMBL4299634 EC50 = 290.0 nM 6.54
CHEMBL4299634 EC50 = 288.4 nM 6.54
CHEMBL3814147 EC50 = 323.59 nM 6.49
CHEMBL3814147 EC50 = 330.0 nM 6.48
CHEMBL4299658 EC50 = 450.0 nM 6.35
CHEMBL4299669 EC50 = 450.0 nM 6.35
CHEMBL4299669 EC50 = 457.09 nM 6.34
CHEMBL4299658 EC50 = 457.09 nM 6.34
CHEMBL3814763 EC50 = 470.0 nM 6.33
CHEMBL3814763 EC50 = 467.74 nM 6.33
CHEMBL3814009 EC50 = 602.56 nM 6.22
CHEMBL3814009 EC50 = 610.0 nM 6.21
CHEMBL3814809 Emax - -
CHEMBL3813825 Emax - -
CHEMBL4299690 Emax - -
CHEMBL4299628 Emax - -
CHEMBL3813751 Emax = 12.4 % -
CHEMBL3814235 Emax - -
CHEMBL3814095 Emax - -
CHEMBL4299627 Emax - -
CHEMBL3814707 Emax - -
CHEMBL3813812 Emax - -
CHEMBL3814492 Emax = 10.8 % -
CHEMBL1742484 Emax = 12.5 % -
CHEMBL3814437 Emax - -
CHEMBL4299652 Emax - -
CHEMBL4299634 Emax = 7.2 % -
CHEMBL3814124 Emax - -
CHEMBL3814092 Emax - -
CHEMBL3814763 Emax = 10.6 % -
CHEMBL4299633 Emax < 3.0 % -
CHEMBL3813773 Emax - -
CHEMBL3814009 Emax = 7.5 % -
CHEMBL4299658 Emax = 3.9 % -
CHEMBL3814437 EC50 < 1000.0 nM -
CHEMBL3814643 EC50 < 1000.0 nM -
CHEMBL4299628 EC50 < 1000.0 nM -
CHEMBL3813812 EC50 < 1000.0 nM -
CHEMBL3814527 EC50 < 1000.0 nM -
CHEMBL3814707 EC50 < 1000.0 nM -