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Assay Detail

CHEMBL3734175

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

Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
70
Total Activities
70
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Imidazothiadiazole derivatives as protease activated receptor 4 (PAR4) inhibitors for treating platelet aggregation
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 70 6.40 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3730431 1 8.30
CHEMBL3730469 1 7.98
CHEMBL3731160 1 7.65
CHEMBL3728620 1 7.61
CHEMBL3731476 1 7.48
CHEMBL3732786 1 7.44
CHEMBL3727781 1 7.42
CHEMBL3731170 1 7.42
CHEMBL3730270 1 7.26
CHEMBL3730494 1 7.18
CHEMBL3733272 1 7.13
CHEMBL3729143 1 7.12
CHEMBL3729253 1 7.07
CHEMBL3731050 1 7.07
CHEMBL3728073 1 7.03
CHEMBL3727965 1 7.02
CHEMBL3732437 1 7.00
CHEMBL3731102 1 6.98
CHEMBL3728013 1 6.96
CHEMBL3732890 1 6.91
CHEMBL3731766 1 6.83
CHEMBL3728008 1 6.82
CHEMBL3732678 1 6.82
CHEMBL3732266 1 6.33
CHEMBL3730712 1 6.26
CHEMBL3731108 1 6.25
CHEMBL3729962 1 6.25
CHEMBL3728638 1 6.24
CHEMBL3728153 1 6.23
CHEMBL3728653 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3730431 IC50 = 4.95 nM 8.30
CHEMBL3730469 IC50 = 10.53 nM 7.98
CHEMBL3731160 IC50 = 22.5 nM 7.65
CHEMBL3728620 IC50 = 24.74 nM 7.61
CHEMBL3731476 IC50 = 33.33 nM 7.48
CHEMBL3732786 IC50 = 36.47 nM 7.44
CHEMBL3727781 IC50 = 38.32 nM 7.42
CHEMBL3731170 IC50 = 37.88 nM 7.42
CHEMBL3730270 IC50 = 54.98 nM 7.26
CHEMBL3730494 IC50 = 66.22 nM 7.18
CHEMBL3733272 IC50 = 73.23 nM 7.13
CHEMBL3729143 IC50 = 75.51 nM 7.12
CHEMBL3729253 IC50 = 86.15 nM 7.07
CHEMBL3731050 IC50 = 85.66 nM 7.07
CHEMBL3728073 IC50 = 93.28 nM 7.03
CHEMBL3727965 IC50 = 95.63 nM 7.02
CHEMBL3732437 IC50 = 101.0 nM 7.00
CHEMBL3731102 IC50 = 105.3 nM 6.98
CHEMBL3728013 IC50 = 108.8 nM 6.96
CHEMBL3732890 IC50 = 124.0 nM 6.91
CHEMBL3731766 IC50 = 146.9 nM 6.83
CHEMBL3728008 IC50 = 150.8 nM 6.82
CHEMBL3732678 IC50 = 150.8 nM 6.82
CHEMBL3732266 IC50 = 462.5 nM 6.33
CHEMBL3730712 IC50 = 544.3 nM 6.26
CHEMBL3731108 IC50 = 568.0 nM 6.25
CHEMBL3729962 IC50 = 566.3 nM 6.25
CHEMBL3728638 IC50 = 579.3 nM 6.24
CHEMBL3728153 IC50 = 594.2 nM 6.23
CHEMBL3728653 IC50 = 615.9 nM 6.21
CHEMBL3727768 IC50 = 677.0 nM 6.17
CHEMBL3731542 IC50 = 2326.0 nM 5.63
CHEMBL3730410 IC50 = 2399.0 nM 5.62
CHEMBL3732797 IC50 = 2495.0 nM 5.60
CHEMBL3728728 IC50 = 2502.0 nM 5.60
CHEMBL3732817 IC50 = 2955.0 nM 5.53
CHEMBL3730719 IC50 = 3083.0 nM 5.51
CHEMBL3730755 IC50 = 3189.0 nM 5.50
CHEMBL3727827 IC50 = 3266.0 nM 5.49
CHEMBL3729435 IC50 = 3413.0 nM 5.47
CHEMBL3732951 IC50 = 5275.0 nM 5.28
CHEMBL3730866 IC50 = 5630.0 nM 5.25
CHEMBL3731888 IC50 = 5818.0 nM 5.24
CHEMBL3727816 IC50 = 6910.0 nM 5.16
CHEMBL3729892 IC50 = 8756.0 nM 5.06
CHEMBL3728563 IC50 = 9164.0 nM 5.04
CHEMBL3731072 IC50 = 9436.0 nM 5.03
CHEMBL3730981 IC50 = 16700.0 nM 4.78
CHEMBL3732594 IC50 > 30000.0 nM -
CHEMBL3730518 IC50 > 30000.0 nM -