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Assay Detail

CHEMBL812833

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Binding
Binding affinity towards thrombin was tested.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Rational design of boropeptide thrombin inhibitors: beta, beta-dialkyl-phenethylglycine P2 analogs of DuP 714 with greater selectivity over complement factor I and an improved safety profile.
Fevig JM, Buriak J, Cacciola J, Alexander RS, Kettner CA, Knabb RM, Pruitt JR, Weber PC, Wexler RR.
Bioorg Med Chem Lett (1998) 8 : 301 -306
PubMed 9871674 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 9.39 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL607008 1 10.40
CHEMBL102385 1 10.22
CHEMBL105137 1 10.22
CHEMBL102916 1 9.55
CHEMBL320213 1 9.52
CHEMBL105212 1 9.44
CHEMBL102779 1 9.43
CHEMBL319050 1 9.39
CHEMBL419734 1 9.38
CHEMBL320019 1 9.37
CHEMBL103078 1 9.28
CHEMBL103077 1 9.24
CHEMBL104331 1 9.08
CHEMBL105393 1 9.05
CHEMBL317639 1 8.92
CHEMBL431056 1 8.62
CHEMBL102930 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL607008 Ki = 0.04 nM 10.40
CHEMBL102385 Ki = 0.06 nM 10.22
CHEMBL105137 Ki = 0.06 nM 10.22
CHEMBL102916 Ki = 0.28 nM 9.55
CHEMBL320213 Ki = 0.3 nM 9.52
CHEMBL105212 Ki = 0.36 nM 9.44
CHEMBL102779 Ki = 0.37 nM 9.43
CHEMBL319050 Ki = 0.41 nM 9.39
CHEMBL419734 Ki = 0.42 nM 9.38
CHEMBL320019 Ki = 0.43 nM 9.37
CHEMBL103078 Ki = 0.53 nM 9.28
CHEMBL103077 Ki = 0.58 nM 9.24
CHEMBL104331 Ki = 0.83 nM 9.08
CHEMBL105393 Ki = 0.89 nM 9.05
CHEMBL317639 Ki = 1.2 nM 8.92
CHEMBL431056 Ki = 2.4 nM 8.62
CHEMBL102930 Ki = 3.0 nM 8.52