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Assay Detail

CHEMBL3721050

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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 before agonist addition by FLIPR assay
ChEMBL ↗
105
Total Activities
105
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 imidazopyridazine derivatives as protease activated receptor 4 (PAR4) inhibitors for treating platelet aggregation
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 105 8.77 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3716902 — — 1 9.64
CHEMBL3715013 — — 1 9.64
CHEMBL3717308 — — 1 9.54
CHEMBL3718355 — — 1 9.51
CHEMBL3717430 — — 1 9.46
CHEMBL3719074 — — 1 9.44
CHEMBL3717518 — — 1 9.44
CHEMBL3714990 — — 1 9.44
CHEMBL3718854 — — 1 9.42
CHEMBL3718880 — — 1 9.41
CHEMBL3716576 — — 1 9.39
CHEMBL3716555 — — 1 9.35
CHEMBL3718564 — — 1 9.33
CHEMBL3719106 — — 1 9.32
CHEMBL3715722 — — 1 9.31
CHEMBL3718990 — — 1 9.30
CHEMBL3716388 — — 1 9.28
CHEMBL3715604 — — 1 9.25
CHEMBL3715826 — — 1 9.25
CHEMBL3716899 — — 1 9.24
CHEMBL3715991 — — 1 9.24
CHEMBL3716636 — — 1 9.22
CHEMBL3717105 — — 1 9.17
CHEMBL3718647 — — 1 9.17
CHEMBL3717597 — — 1 9.16
CHEMBL3717959 — — 1 9.16
CHEMBL3716460 — — 1 9.16
CHEMBL3716332 — — 1 9.15
CHEMBL3717220 — — 1 9.14
CHEMBL3716464 — — 1 9.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3716902 — IC50 = 0.23 nM 9.64
CHEMBL3715013 — IC50 = 0.23 nM 9.64
CHEMBL3717308 — IC50 = 0.29 nM 9.54
CHEMBL3718355 — IC50 = 0.31 nM 9.51
CHEMBL3717430 — IC50 = 0.35 nM 9.46
CHEMBL3717518 — IC50 = 0.36 nM 9.44
CHEMBL3714990 — IC50 = 0.36 nM 9.44
CHEMBL3719074 — IC50 = 0.36 nM 9.44
CHEMBL3718854 — IC50 = 0.38 nM 9.42
CHEMBL3718880 — IC50 = 0.39 nM 9.41
CHEMBL3716576 — IC50 = 0.41 nM 9.39
CHEMBL3716555 — IC50 = 0.45 nM 9.35
CHEMBL3718564 — IC50 = 0.47 nM 9.33
CHEMBL3719106 — IC50 = 0.48 nM 9.32
CHEMBL3715722 — IC50 = 0.49 nM 9.31
CHEMBL3718990 — IC50 = 0.5 nM 9.30
CHEMBL3716388 — IC50 = 0.53 nM 9.28
CHEMBL3715826 — IC50 = 0.56 nM 9.25
CHEMBL3715604 — IC50 = 0.56 nM 9.25
CHEMBL3715991 — IC50 = 0.57 nM 9.24
CHEMBL3716899 — IC50 = 0.57 nM 9.24
CHEMBL3716636 — IC50 = 0.6 nM 9.22
CHEMBL3717105 — IC50 = 0.67 nM 9.17
CHEMBL3718647 — IC50 = 0.68 nM 9.17
CHEMBL3717959 — IC50 = 0.69 nM 9.16
CHEMBL3717597 — IC50 = 0.69 nM 9.16
CHEMBL3716460 — IC50 = 0.69 nM 9.16
CHEMBL3716332 — IC50 = 0.71 nM 9.15
CHEMBL3717220 — IC50 = 0.72 nM 9.14
CHEMBL3716464 — IC50 = 0.72 nM 9.14
CHEMBL3716818 — IC50 = 0.74 nM 9.13
CHEMBL3717703 — IC50 = 0.76 nM 9.12
CHEMBL3715717 — IC50 = 0.79 nM 9.10
CHEMBL3716397 — IC50 = 0.84 nM 9.08
CHEMBL3719049 — IC50 = 0.85 nM 9.07
CHEMBL3719264 — IC50 = 0.92 nM 9.04
CHEMBL3718901 — IC50 = 0.95 nM 9.02
CHEMBL3719244 — IC50 = 1.0 nM 9.00
CHEMBL3716502 — IC50 = 1.03 nM 8.99
CHEMBL3714996 — IC50 = 1.03 nM 8.99
CHEMBL3715007 — IC50 = 1.05 nM 8.98
CHEMBL3719331 — IC50 = 1.06 nM 8.97
CHEMBL3715775 — IC50 = 1.06 nM 8.97
CHEMBL3717838 — IC50 = 1.08 nM 8.97
CHEMBL3717026 — IC50 = 1.11 nM 8.96
CHEMBL3719340 — IC50 = 1.09 nM 8.96
CHEMBL3716323 — IC50 = 1.1 nM 8.96
CHEMBL3715416 — IC50 = 1.21 nM 8.92
CHEMBL3718187 — IC50 = 1.19 nM 8.92
CHEMBL3716344 — IC50 = 1.22 nM 8.91