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Assay Detail

CHEMBL4835313

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

Binding
Inhibition of recombinant human activated TAFI incubated for 45 mins using hippuryl-arginine as substrate by spectrophotometry
56
Total Activities
55
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Carboxypeptidase B2 (CHEMBL3419)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Phosphinanes and Azaphosphinanes as Potent and Selective Inhibitors of Activated Thrombin-Activatable Fibrinolysis Inhibitor (TAFIa).
Schaffner AP, Sansilvestri-Morel P, Despaux N, Ruano E, Persigand T, Rupin A, Mennecier P, Vallez MO, Raimbaud E, Desos P, Gloanec P.
J Med Chem (2021) 64 : 3897 -3910
PubMed 33764059 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 55 6.62 9.00
Ki 1 9.12 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4878039 2 9.12
CHEMBL4868605 1 9.00
CHEMBL4846664 1 8.70
CHEMBL4858095 1 8.30
CHEMBL4861532 1 8.30
CHEMBL4853133 1 8.15
CHEMBL4852722 1 8.10
CHEMBL4858909 1 8.10
CHEMBL4875723 1 8.05
CHEMBL4852607 1 8.05
CHEMBL4861840 1 8.00
CHEMBL4854445 1 7.96
CHEMBL4866725 1 7.77
CHEMBL4868496 1 7.51
CHEMBL4858525 1 7.06
CHEMBL4861694 1 7.00
CHEMBL4856598 1 7.00
CHEMBL4846016 1 6.90
CHEMBL4855391 1 6.79
CHEMBL4847492 1 6.74
CHEMBL4869435 1 6.70
CHEMBL4862631 1 6.70
CHEMBL4857164 1 6.70
CHEMBL4861443 1 6.30
CHEMBL4855720 1 6.30
CHEMBL4848798 1 6.29
CHEMBL4864051 1 6.12
CHEMBL4858857 1 5.96
CHEMBL4851707 1 5.96
CHEMBL4879366 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4878039 Ki = 0.75 nM 9.12
CHEMBL4868605 IC50 = 1.0 nM 9.00
CHEMBL4846664 IC50 = 2.0 nM 8.70
CHEMBL4861532 IC50 = 5.0 nM 8.30
CHEMBL4858095 IC50 = 5.0 nM 8.30
CHEMBL4878039 IC50 = 6.0 nM 8.22
CHEMBL4853133 IC50 = 7.0 nM 8.15
CHEMBL4858909 IC50 = 8.0 nM 8.10
CHEMBL4852722 IC50 = 8.0 nM 8.10
CHEMBL4852607 IC50 = 9.0 nM 8.05
CHEMBL4875723 IC50 = 9.0 nM 8.05
CHEMBL4861840 IC50 = 10.0 nM 8.00
CHEMBL4854445 IC50 = 11.0 nM 7.96
CHEMBL4866725 IC50 = 17.0 nM 7.77
CHEMBL4868496 IC50 = 31.0 nM 7.51
CHEMBL4858525 IC50 = 87.0 nM 7.06
CHEMBL4861694 IC50 = 101.0 nM 7.00
CHEMBL4856598 IC50 = 100.0 nM 7.00
CHEMBL4846016 IC50 = 127.0 nM 6.90
CHEMBL4855391 IC50 = 161.0 nM 6.79
CHEMBL4847492 IC50 = 183.0 nM 6.74
CHEMBL4857164 IC50 = 200.0 nM 6.70
CHEMBL4869435 IC50 = 200.0 nM 6.70
CHEMBL4862631 IC50 = 200.0 nM 6.70
CHEMBL4855720 IC50 = 500.0 nM 6.30
CHEMBL4861443 IC50 = 500.0 nM 6.30
CHEMBL4848798 IC50 = 515.0 nM 6.29
CHEMBL4864051 IC50 = 750.0 nM 6.12
CHEMBL4851707 IC50 = 1100.0 nM 5.96
CHEMBL4858857 IC50 = 1100.0 nM 5.96
CHEMBL4879366 IC50 = 1500.0 nM 5.82
CHEMBL4861262 IC50 = 1500.0 nM 5.82
CHEMBL4877745 IC50 = 1800.0 nM 5.75
CHEMBL4851494 IC50 = 2600.0 nM 5.58
CHEMBL4850188 IC50 = 3104.0 nM 5.51
CHEMBL4860221 IC50 = 5000.0 nM 5.30
CHEMBL4850416 IC50 = 5000.0 nM 5.30
CHEMBL4868220 IC50 = 8000.0 nM 5.10
CHEMBL4872299 IC50 = 8700.0 nM 5.06
CHEMBL4865984 IC50 = 9300.0 nM 5.03
CHEMBL4864497 IC50 = 10700.0 nM 4.97
CHEMBL4878365 IC50 = 11700.0 nM 4.93
CHEMBL4871500 IC50 = 18000.0 nM 4.75
CHEMBL4856209 IC50 = 19000.0 nM 4.72
CHEMBL4877082 IC50 = 20100.0 nM 4.70
CHEMBL4857886 IC50 > 30000.0 nM -
CHEMBL4848329 IC50 > 30000.0 nM -
CHEMBL4864625 IC50 > 30000.0 nM -
CHEMBL4867193 IC50 > 30000.0 nM -
CHEMBL4870502 IC50 > 30000.0 nM -