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Assay Detail

CHEMBL2320212

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

Binding
Inhibition of human thrombin using CH3SO2-D-Cha-Gly-Arg-pNA as substrate after 5 to 10 mins by micro plate reader analysis
14
Total Activities
14
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

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of new cyclic plasmin inhibitors with excellent potency and selectivity.
Saupe SM, Leubner S, Betz M, Klebe G, Steinmetzer T.
J Med Chem (2013) 56 : 820 -831
PubMed 23294255 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 5.42 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2315240 1 6.64
CHEMBL2315245 1 6.42
CHEMBL2315242 1 6.22
CHEMBL2315236 1 6.05
CHEMBL2315238 1 5.53
CHEMBL2315244 1 5.49
CHEMBL2315237 1 5.23
CHEMBL2315241 1 5.10
CHEMBL2315235 1 5.07
CHEMBL2315247 1 4.95
CHEMBL2315234 1 4.92
CHEMBL2315239 1 4.86
CHEMBL2315246 1 4.85
CHEMBL2315243 1 4.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2315240 Ki = 227.0 nM 6.64
CHEMBL2315245 Ki = 376.0 nM 6.42
CHEMBL2315242 Ki = 604.0 nM 6.22
CHEMBL2315236 Ki = 884.0 nM 6.05
CHEMBL2315238 Ki = 2950.0 nM 5.53
CHEMBL2315244 Ki = 3250.0 nM 5.49
CHEMBL2315237 Ki = 5870.0 nM 5.23
CHEMBL2315241 Ki = 8017.0 nM 5.10
CHEMBL2315235 Ki = 8510.0 nM 5.07
CHEMBL2315247 Ki = 11210.0 nM 4.95
CHEMBL2315234 Ki = 12082.0 nM 4.92
CHEMBL2315239 Ki = 13870.0 nM 4.86
CHEMBL2315246 Ki = 14143.0 nM 4.85
CHEMBL2315243 Ki = 26420.0 nM 4.58