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Assay Detail

CHEMBL5355148

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Functional
Inhibition of thrombin induced platelet activation in CD-1 mouse plasma incubated for 2 mins by luminescence based assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Tissue Plasma
Cell Type Platelet
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of novel N-acylpyrazoles as potent and selective thrombin inhibitors.
Short KM, Estiarte MA, Pham SM, Williams DC, Igoudin L, Dash S, Sandoval N, Datta A, Pozzi N, Di Cera E, Kita DB.
Eur J Med Chem (2023) 246 : 114855 -114855
PubMed 36462436 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.20 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502016 1 8.15
CHEMBL48361 DABIGATRAN 3.0 1 8.15
CHEMBL5397791 1 5.36
CHEMBL5421979 1 4.96
CHEMBL5397575 1 4.37
CHEMBL198362 RIVAROXABAN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502016 EC50 = 7.0 nM 8.15
CHEMBL48361 DABIGATRAN EC50 = 7.0 nM 8.15
CHEMBL5397791 EC50 = 4400.0 nM 5.36
CHEMBL5421979 EC50 = 11000.0 nM 4.96
CHEMBL5397575 EC50 = 43000.0 nM 4.37
CHEMBL198362 RIVAROXABAN EC50 > 10000.0 nM -