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Assay Detail

CHEMBL811966

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Binding
Inhibition of thrombin in human plasma
15
Total Activities
15
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 Expert

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'.
Sanderson PE, Cutrona KJ, Dyer DL, Krueger JA, Kuo LC, Lewis SD, Lucas BJ, Yan Y.
Bioorg Med Chem Lett (2003) 13 : 161 -164
PubMed 12482415 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.05 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296737 1 10.40
CHEMBL431524 1 10.15
CHEMBL42039 1 9.13
CHEMBL19080 L-375378 1 9.10
CHEMBL42495 1 8.30
CHEMBL296041 1 8.15
CHEMBL44226 1 8.13
CHEMBL45062 1 8.07
CHEMBL46638 1 7.92
CHEMBL43641 1 7.82
CHEMBL43145 1 7.75
CHEMBL42091 1 7.62
CHEMBL44249 1 6.47
CHEMBL44868 1 6.05
CHEMBL42496 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296737 Ki = 0.04 nM 10.40
CHEMBL431524 Ki = 0.07 nM 10.15
CHEMBL42039 Ki = 0.74 nM 9.13
CHEMBL19080 L-375378 Ki = 0.8 nM 9.10
CHEMBL42495 Ki = 5.0 nM 8.30
CHEMBL296041 Ki = 7.0 nM 8.15
CHEMBL44226 Ki = 7.4 nM 8.13
CHEMBL45062 Ki = 8.5 nM 8.07
CHEMBL46638 Ki = 12.0 nM 7.92
CHEMBL43641 Ki = 15.0 nM 7.82
CHEMBL43145 Ki = 18.0 nM 7.75
CHEMBL42091 Ki = 24.0 nM 7.62
CHEMBL44249 Ki = 340.0 nM 6.47
CHEMBL44868 Ki = 900.0 nM 6.05
CHEMBL42496 Ki = 2100.0 nM 5.68