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Assay Detail

CHEMBL3580143

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

Binding
Inhibition of human activated TAFI incubated for 15 mins by microtiter plate reader based assay
42
Total Activities
42
Compounds Tested
1
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

Novel Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa) from Natural Product Anabaenopeptin.
Halland N, Brönstrup M, Czech J, Czechtizky W, Evers A, Follmann M, Kohlmann M, Schiell M, Kurz M, Schreuder HA, Kallus C.
J Med Chem (2015) 58 : 4839 -4844
PubMed 25990761 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 6.98 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3577442 1 9.00
CHEMBL175436 ANABAENOPEPTIN F 1 8.82
CHEMBL368684 ANABAENOPEPTIN B 1 8.82
CHEMBL3577334 1 8.72
CHEMBL3577425 1 8.52
CHEMBL3577435 1 8.40
CHEMBL3577440 1 8.40
CHEMBL3577439 1 8.40
CHEMBL3577433 1 8.15
CHEMBL3577434 1 8.05
CHEMBL3577432 1 7.82
CHEMBL3577426 1 7.82
CHEMBL3577436 1 7.75
CHEMBL3577336 1 7.72
CHEMBL3577335 1 7.51
CHEMBL3577438 1 7.42
CHEMBL3577424 1 7.41
CHEMBL3577427 1 7.24
CHEMBL3577441 1 7.00
CHEMBL3577437 1 6.96
CHEMBL3577423 1 6.96
CHEMBL3577337 1 6.92
CHEMBL3577325 1 6.89
CHEMBL3577330 1 6.77
CHEMBL3577329 1 6.72
CHEMBL3577443 1 6.60
CHEMBL3577326 1 6.41
CHEMBL446236 OSCILLAMIDE Y 1 6.40
CHEMBL3577428 1 6.34
CHEMBL3577445 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3577442 IC50 = 1.0 nM 9.00
CHEMBL175436 ANABAENOPEPTIN F IC50 = 1.5 nM 8.82
CHEMBL368684 ANABAENOPEPTIN B IC50 = 1.5 nM 8.82
CHEMBL3577334 IC50 = 1.9 nM 8.72
CHEMBL3577425 IC50 = 3.0 nM 8.52
CHEMBL3577435 IC50 = 4.0 nM 8.40
CHEMBL3577440 IC50 = 4.0 nM 8.40
CHEMBL3577439 IC50 = 4.0 nM 8.40
CHEMBL3577433 IC50 = 7.0 nM 8.15
CHEMBL3577434 IC50 = 9.0 nM 8.05
CHEMBL3577432 IC50 = 15.0 nM 7.82
CHEMBL3577426 IC50 = 15.0 nM 7.82
CHEMBL3577436 IC50 = 18.0 nM 7.75
CHEMBL3577336 IC50 = 19.0 nM 7.72
CHEMBL3577335 IC50 = 31.0 nM 7.51
CHEMBL3577438 IC50 = 38.0 nM 7.42
CHEMBL3577424 IC50 = 39.0 nM 7.41
CHEMBL3577427 IC50 = 57.0 nM 7.24
CHEMBL3577441 IC50 = 100.0 nM 7.00
CHEMBL3577437 IC50 = 110.0 nM 6.96
CHEMBL3577423 IC50 = 110.0 nM 6.96
CHEMBL3577337 IC50 = 120.0 nM 6.92
CHEMBL3577325 IC50 = 130.0 nM 6.89
CHEMBL3577330 IC50 = 170.0 nM 6.77
CHEMBL3577329 IC50 = 190.0 nM 6.72
CHEMBL3577443 IC50 = 250.0 nM 6.60
CHEMBL3577326 IC50 = 390.0 nM 6.41
CHEMBL446236 OSCILLAMIDE Y IC50 = 400.0 nM 6.40
CHEMBL3577428 IC50 = 460.0 nM 6.34
CHEMBL3577445 IC50 = 570.0 nM 6.24
CHEMBL3577327 IC50 = 690.0 nM 6.16
CHEMBL3577444 IC50 = 750.0 nM 6.12
CHEMBL3577328 IC50 = 850.0 nM 6.07
CHEMBL3577338 IC50 = 900.0 nM 6.05
CHEMBL3577429 IC50 = 1000.0 nM 6.00
CHEMBL3577422 IC50 = 1200.0 nM 5.92
CHEMBL3577333 IC50 = 1400.0 nM 5.85
CHEMBL3577332 IC50 = 1500.0 nM 5.82
CHEMBL3577430 IC50 = 3700.0 nM 5.43
CHEMBL3577431 IC50 = 6100.0 nM 5.21
CHEMBL3577446 IC50 = 54000.0 nM 4.27
CHEMBL3577331 IC50 = 59000.0 nM 4.23