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Assay Detail

CHEMBL3706209

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Binding
Inhibition Assay: The prepared substances were tested for TAFIa inhibition using the Actichrome plasma TAFI activity kit from American Diagnostica (Pr. No. 874). This entailed adding 29 μl of assay buffer (20 mM Hepes, 150 mM NaCl, pH 7.4) and 10 μl of TAFIa (American Diagnostica Pr. No. 874TAFIA; 2.5/ml) to 1 μl of 5 mM DMSO solution of the substance and incubating in a 96 half-well microtiter plate at room temperature for 15 minutes. The enzymic reaction was started by adding 10 μl of TAFIa developer (prediluted 1:2 with water). The time course of the reaction was followed at 420 nm in a microtiter plate reader (SpectraMax plus 384; Molecular Devices) for 15 minutes.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Carboxypeptidase B (CHEMBL2552)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Imidazole derivatives used as TAFIa inhibitors
(2014)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.10 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3694281 1 8.52
CHEMBL3694275 1 7.96
CHEMBL3694272 1 7.92
CHEMBL3694273 1 7.92
CHEMBL3694271 1 7.82
CHEMBL3694267 1 7.80
CHEMBL3694276 1 7.68
CHEMBL3694270 1 7.64
CHEMBL3694266 1 7.52
CHEMBL3694274 1 7.42
CHEMBL3694282 1 7.31
CHEMBL3694269 1 6.36
CHEMBL3694280 1 6.06
CHEMBL3694278 1 5.96
CHEMBL3694268 1 5.95
CHEMBL3694279 1 5.84
CHEMBL3694277 1 4.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3694281 IC50 = 3.0 nM 8.52
CHEMBL3694275 IC50 = 11.0 nM 7.96
CHEMBL3694272 IC50 = 12.0 nM 7.92
CHEMBL3694273 IC50 = 12.0 nM 7.92
CHEMBL3694271 IC50 = 15.0 nM 7.82
CHEMBL3694267 IC50 = 16.0 nM 7.80
CHEMBL3694276 IC50 = 21.0 nM 7.68
CHEMBL3694270 IC50 = 23.0 nM 7.64
CHEMBL3694266 IC50 = 30.0 nM 7.52
CHEMBL3694274 IC50 = 38.0 nM 7.42
CHEMBL3694282 IC50 = 49.0 nM 7.31
CHEMBL3694269 IC50 = 439.0 nM 6.36
CHEMBL3694280 IC50 = 870.0 nM 6.06
CHEMBL3694278 IC50 = 1110.0 nM 5.96
CHEMBL3694268 IC50 = 1130.0 nM 5.95
CHEMBL3694279 IC50 = 1440.0 nM 5.84
CHEMBL3694277 IC50 = 10510.0 nM 4.98