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Assay Detail

CHEMBL3721139

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Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL ↗
310
Total Activities
310
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Proteinase-activated receptor 4 (CHEMBL4691) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Imidazothiadiazole and imidazopyrazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 310 8.96 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3715479 — — 1 9.74
CHEMBL3718225 — — 1 9.68
CHEMBL3716420 — — 1 9.64
CHEMBL3716230 — — 1 9.62
CHEMBL3717127 — — 1 9.60
CHEMBL3718763 — — 1 9.59
CHEMBL3717042 — — 1 9.59
CHEMBL3717235 — — 1 9.59
CHEMBL3717808 — — 1 9.59
CHEMBL3715840 — — 1 9.59
CHEMBL3718631 — — 1 9.57
CHEMBL3716142 — — 1 9.57
CHEMBL3718707 — — 1 9.57
CHEMBL3717618 — — 1 9.57
CHEMBL3717706 — — 1 9.55
CHEMBL3715442 — — 1 9.54
CHEMBL3716059 — — 1 9.54
CHEMBL3715043 — — 1 9.52
CHEMBL3717937 — — 1 9.52
CHEMBL3718801 — — 1 9.51
CHEMBL3715853 — — 1 9.51
CHEMBL3714842 — — 1 9.51
CHEMBL3717419 — — 1 9.49
CHEMBL3718267 — — 1 9.49
CHEMBL3717956 — — 1 9.49
CHEMBL3716160 — — 1 9.49
CHEMBL3715848 — — 1 9.49
CHEMBL3716904 — — 1 9.48
CHEMBL3716623 — — 1 9.48
CHEMBL3718639 — — 1 9.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3715479 — EC50 = 0.18 nM 9.74
CHEMBL3718225 — EC50 = 0.21 nM 9.68
CHEMBL3716420 — EC50 = 0.23 nM 9.64
CHEMBL3716230 — EC50 = 0.24 nM 9.62
CHEMBL3717127 — EC50 = 0.25 nM 9.60
CHEMBL3715840 — EC50 = 0.26 nM 9.59
CHEMBL3717235 — EC50 = 0.26 nM 9.59
CHEMBL3717042 — EC50 = 0.26 nM 9.59
CHEMBL3717808 — EC50 = 0.26 nM 9.59
CHEMBL3718763 — EC50 = 0.26 nM 9.59
CHEMBL3718631 — EC50 = 0.27 nM 9.57
CHEMBL3716142 — EC50 = 0.27 nM 9.57
CHEMBL3718707 — EC50 = 0.27 nM 9.57
CHEMBL3717618 — EC50 = 0.27 nM 9.57
CHEMBL3717706 — EC50 = 0.28 nM 9.55
CHEMBL3716059 — EC50 = 0.29 nM 9.54
CHEMBL3715442 — EC50 = 0.29 nM 9.54
CHEMBL3717937 — EC50 = 0.3 nM 9.52
CHEMBL3715043 — EC50 = 0.3 nM 9.52
CHEMBL3715853 — EC50 = 0.31 nM 9.51
CHEMBL3718801 — EC50 = 0.31 nM 9.51
CHEMBL3714842 — EC50 = 0.31 nM 9.51
CHEMBL3718267 — EC50 = 0.32 nM 9.49
CHEMBL3717419 — EC50 = 0.32 nM 9.49
CHEMBL3716160 — EC50 = 0.32 nM 9.49
CHEMBL3715848 — EC50 = 0.32 nM 9.49
CHEMBL3717956 — EC50 = 0.32 nM 9.49
CHEMBL3716904 — EC50 = 0.33 nM 9.48
CHEMBL3715876 — EC50 = 0.33 nM 9.48
CHEMBL3716723 — EC50 = 0.33 nM 9.48
CHEMBL3716623 — EC50 = 0.33 nM 9.48
CHEMBL3718639 — EC50 = 0.33 nM 9.48
CHEMBL3714941 — EC50 = 0.34 nM 9.47
CHEMBL3718692 — EC50 = 0.34 nM 9.47
CHEMBL3715557 — EC50 = 0.34 nM 9.47
CHEMBL3716638 — EC50 = 0.35 nM 9.46
CHEMBL3716290 — EC50 = 0.36 nM 9.44
CHEMBL3716986 — EC50 = 0.36 nM 9.44
CHEMBL3719256 — EC50 = 0.36 nM 9.44
CHEMBL3719034 — EC50 = 0.36 nM 9.44
CHEMBL3716763 — EC50 = 0.37 nM 9.43
CHEMBL3716144 — EC50 = 0.37 nM 9.43
CHEMBL3715900 — EC50 = 0.37 nM 9.43
CHEMBL3719085 — EC50 = 0.37 nM 9.43
CHEMBL3717435 — EC50 = 0.37 nM 9.43
CHEMBL3715066 — EC50 = 0.38 nM 9.42
CHEMBL3716212 — EC50 = 0.38 nM 9.42
CHEMBL3718540 — EC50 = 0.39 nM 9.41
CHEMBL3716844 — EC50 = 0.4 nM 9.40
CHEMBL3718152 — EC50 = 0.4 nM 9.40