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Assay Detail

CHEMBL5148581

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

Functional
Antiplatelet activity in human platelet-rich plasma assessed as inhibition of gamma thrombin induced platelet aggregation preincubated for 5 mins followed by gamma thrombin addition and measured upto 15 mins by plate reader assay
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Plasma
Cell Type Platelet
Confidence 1 — Organism
Curated By Autocuration

Target

Plasma (CHEMBL613424)
Type TISSUE
Organism Homo sapiens

Publication

Discovery of Two Novel Antiplatelet Clinical Candidates (BMS-986120 and BMS-986141) That Antagonize Protease-Activated Receptor 4.
Priestley ES, Banville J, Deon D, Dubé L, Gagnon M, Guy J, Lapointe P, Lavallée JF, Martel A, Plamondon S, Rémillard R, Ruediger E, Tremblay F, Posy SL, Guarino VR, Richter JM, Li J, Gupta A, Vetrichelvan M, Balapragalathan TJ, Mathur A, Hua J, Callejo M, Guay J, Sum CS, Cvijic ME, Watson C, Wong P, Yang J, Bouvier M, Gordon DA, Wexler RR, Marinier A.
J Med Chem (2022) 65 : 8843 -8854
PubMed 35729784 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 53 7.63 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5173906 1 9.10
CHEMBL3715264 1 8.96
CHEMBL3717580 1 8.82
CHEMBL3715516 1 8.80
CHEMBL3718360 1 8.72
CHEMBL3716552 BMS-986141 2.0 1 8.68
CHEMBL5194507 1 8.55
CHEMBL3718564 1 8.54
CHEMBL3716064 1 8.52
CHEMBL3717275 1 8.44
CHEMBL3719133 1 8.41
CHEMBL5193311 1 8.40
CHEMBL3715840 1 8.36
CHEMBL3715848 1 8.33
CHEMBL3717195 1 8.24
CHEMBL3716066 1 8.17
CHEMBL3716726 1 8.12
CHEMBL3719069 1 8.08
CHEMBL3717535 1 8.04
CHEMBL3719106 1 8.01
CHEMBL3718231 1 8.01
CHEMBL3716636 1 8.00
CHEMBL3715632 1 7.96
CHEMBL3719264 1 7.92
CHEMBL3717597 1 7.92
CHEMBL3717937 1 7.92
CHEMBL3719215 1 7.80
CHEMBL3717235 1 7.75
CHEMBL3717040 1 7.75
CHEMBL3716230 1 7.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5173906 IC50 = 0.8 nM 9.10
CHEMBL3715264 IC50 = 1.1 nM 8.96
CHEMBL3717580 IC50 = 1.5 nM 8.82
CHEMBL3715516 IC50 = 1.6 nM 8.80
CHEMBL3718360 IC50 = 1.9 nM 8.72
CHEMBL3716552 BMS-986141 IC50 = 2.1 nM 8.68
CHEMBL5194507 IC50 = 2.8 nM 8.55
CHEMBL3718564 IC50 = 2.9 nM 8.54
CHEMBL3716064 IC50 = 3.0 nM 8.52
CHEMBL3717275 IC50 = 3.6 nM 8.44
CHEMBL3719133 IC50 = 3.9 nM 8.41
CHEMBL5193311 IC50 = 4.0 nM 8.40
CHEMBL3715840 IC50 = 4.4 nM 8.36
CHEMBL3715848 IC50 = 4.7 nM 8.33
CHEMBL3717195 IC50 = 5.7 nM 8.24
CHEMBL3716066 IC50 = 6.7 nM 8.17
CHEMBL3716726 IC50 = 7.6 nM 8.12
CHEMBL3719069 IC50 = 8.4 nM 8.08
CHEMBL3717535 IC50 = 9.2 nM 8.04
CHEMBL3719106 IC50 = 9.8 nM 8.01
CHEMBL3718231 IC50 = 9.7 nM 8.01
CHEMBL3716636 IC50 = 10.0 nM 8.00
CHEMBL3715632 IC50 = 11.0 nM 7.96
CHEMBL3717937 IC50 = 12.0 nM 7.92
CHEMBL3719264 IC50 = 12.0 nM 7.92
CHEMBL3717597 IC50 = 12.0 nM 7.92
CHEMBL3719215 IC50 = 16.0 nM 7.80
CHEMBL3717235 IC50 = 18.0 nM 7.75
CHEMBL3717040 IC50 = 18.0 nM 7.75
CHEMBL3716230 IC50 = 22.0 nM 7.66
CHEMBL3714821 IC50 = 22.0 nM 7.66
CHEMBL5177223 IC50 = 25.0 nM 7.60
CHEMBL3728620 IC50 = 25.0 nM 7.60
CHEMBL3718639 IC50 = 28.0 nM 7.55
CHEMBL3715722 IC50 = 38.0 nM 7.42
CHEMBL3715093 IC50 = 39.0 nM 7.41
CHEMBL3719331 IC50 = 44.0 nM 7.36
CHEMBL5189522 IC50 = 56.0 nM 7.25
CHEMBL3718059 IC50 = 63.0 nM 7.20
CHEMBL5206095 IC50 = 74.0 nM 7.13
CHEMBL3716950 IC50 = 93.0 nM 7.03
CHEMBL3718313 IC50 = 150.0 nM 6.82
CHEMBL5184586 IC50 = 150.0 nM 6.82
CHEMBL3718606 IC50 = 280.0 nM 6.55
CHEMBL3715852 IC50 = 310.0 nM 6.51
CHEMBL3718163 IC50 = 620.0 nM 6.21
CHEMBL5206065 IC50 = 900.0 nM 6.05
CHEMBL3715642 IC50 = 1100.0 nM 5.96
CHEMBL5205126 IC50 = 1300.0 nM 5.89
CHEMBL3732490 IC50 = 1600.0 nM 5.80