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Assay Detail

CHEMBL5355131

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

Functional
Anticoagulant activity in human platelet-poor plasma assessed as endogenous thrombin potential by measuring released free thrombin level incubated for 90 mins in presence of Z-GGR-AMC and CaCl2 by fluorescence based analysis
ChEMBL ↗
71
Total Activities
70
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Plasma (CHEMBL613424) ↗
Type TISSUE
Organism Homo sapiens

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 70 5.14 6.52
EC98 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL48361 DABIGATRAN 3.0 1 6.52
CHEMBL198362 RIVAROXABAN 4.0 1 6.51
CHEMBL502016 — — 1 6.44
CHEMBL266349 MELAGATRAN 4.0 1 6.40
CHEMBL5423783 — — 1 5.89
CHEMBL1373768 — — 1 5.85
CHEMBL5418843 — — 1 5.77
CHEMBL5425314 — — 2 5.75
CHEMBL5435750 — — 1 5.75
CHEMBL5423794 — — 1 5.66
CHEMBL5410218 — — 1 5.64
CHEMBL5425205 — — 1 5.57
CHEMBL5429011 — — 1 5.55
CHEMBL5423051 — — 1 5.47
CHEMBL5428035 — — 1 5.47
CHEMBL5427798 — — 1 5.40
CHEMBL5421979 — — 1 5.39
CHEMBL5397791 — — 1 5.39
CHEMBL5402462 — — 1 5.34
CHEMBL5409763 — — 1 5.33
CHEMBL5437092 — — 1 5.29
CHEMBL5399103 — — 1 5.27
CHEMBL5395380 — — 1 5.19
CHEMBL5410746 — — 1 5.17
CHEMBL5426345 — — 1 5.16
CHEMBL5409452 — — 1 5.16
CHEMBL5424533 — — 1 5.09
CHEMBL5426702 — — 1 5.08
CHEMBL5428720 — — 1 5.07
CHEMBL5397575 — — 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL48361 DABIGATRAN EC50 = 300.0 nM 6.52
CHEMBL198362 RIVAROXABAN EC50 = 310.0 nM 6.51
CHEMBL502016 — EC50 = 360.0 nM 6.44
CHEMBL266349 MELAGATRAN EC50 = 400.0 nM 6.40
CHEMBL5423783 — EC50 = 1300.0 nM 5.89
CHEMBL1373768 — EC50 = 1400.0 nM 5.85
CHEMBL5418843 — EC50 = 1700.0 nM 5.77
CHEMBL5425314 — EC50 = 1800.0 nM 5.75
CHEMBL5435750 — EC50 = 1800.0 nM 5.75
CHEMBL5423794 — EC50 = 2200.0 nM 5.66
CHEMBL5410218 — EC50 = 2300.0 nM 5.64
CHEMBL5425205 — EC50 = 2700.0 nM 5.57
CHEMBL5429011 — EC50 = 2800.0 nM 5.55
CHEMBL5428035 — EC50 = 3400.0 nM 5.47
CHEMBL5423051 — EC50 = 3400.0 nM 5.47
CHEMBL5427798 — EC50 = 4000.0 nM 5.40
CHEMBL5421979 — EC50 = 4100.0 nM 5.39
CHEMBL5397791 — EC50 = 4100.0 nM 5.39
CHEMBL5402462 — EC50 = 4600.0 nM 5.34
CHEMBL5409763 — EC50 = 4700.0 nM 5.33
CHEMBL5437092 — EC50 = 5100.0 nM 5.29
CHEMBL5399103 — EC50 = 5400.0 nM 5.27
CHEMBL5395380 — EC50 = 6400.0 nM 5.19
CHEMBL5410746 — EC50 = 6800.0 nM 5.17
CHEMBL5426345 — EC50 = 6900.0 nM 5.16
CHEMBL5409452 — EC50 = 6900.0 nM 5.16
CHEMBL5424533 — EC50 = 8200.0 nM 5.09
CHEMBL5426702 — EC50 = 8300.0 nM 5.08
CHEMBL5397575 — EC50 = 8500.0 nM 5.07
CHEMBL5428720 — EC50 = 8600.0 nM 5.07
CHEMBL5440166 — EC50 = 8800.0 nM 5.06
CHEMBL5400494 — EC50 = 11000.0 nM 4.96
CHEMBL5406565 — EC50 = 11000.0 nM 4.96
CHEMBL5404585 — EC50 = 11000.0 nM 4.96
CHEMBL5439917 — EC50 = 11000.0 nM 4.96
CHEMBL5418276 — EC50 = 13000.0 nM 4.89
CHEMBL5420677 — EC50 = 18000.0 nM 4.75
CHEMBL5423577 — EC50 = 18000.0 nM 4.75
CHEMBL5439706 — EC50 = 22000.0 nM 4.66
CHEMBL5424963 — EC50 = 23000.0 nM 4.64
CHEMBL5410338 — EC50 = 24000.0 nM 4.62
CHEMBL5401837 — EC50 = 26000.0 nM 4.58
CHEMBL5412218 — EC50 = 30000.0 nM 4.52
CHEMBL5430493 — EC50 = 31000.0 nM 4.51
CHEMBL5411345 — EC50 = 31000.0 nM 4.51
CHEMBL5399192 — EC50 = 32000.0 nM 4.50
CHEMBL5397540 — EC50 = 32000.0 nM 4.50
CHEMBL5427575 — EC50 = 42000.0 nM 4.38
CHEMBL5428764 — EC50 = 46000.0 nM 4.34
CHEMBL5396060 — EC50 = 49000.0 nM 4.31