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Assay Detail

CHEMBL817807

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Binding
Inhibition of trypsin 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 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Trypsin (CHEMBL2095204)
Type PROTEIN FAMILY
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 4.98 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL431524 1 6.00
CHEMBL19080 L-375378 1 5.75
CHEMBL296737 1 5.70
CHEMBL43641 1 5.15
CHEMBL46638 1 5.14
CHEMBL45062 1 5.00
CHEMBL44226 1 4.96
CHEMBL43145 1 4.85
CHEMBL44249 1 4.70
CHEMBL296041 1 4.70
CHEMBL42039 1 4.64
CHEMBL44868 1 4.64
CHEMBL42495 1 4.54
CHEMBL42091 1 4.00
CHEMBL42496 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL431524 Ki = 1000.0 nM 6.00
CHEMBL19080 L-375378 Ki = 1800.0 nM 5.75
CHEMBL296737 Ki = 2000.0 nM 5.70
CHEMBL43641 Ki = 7100.0 nM 5.15
CHEMBL46638 Ki = 7200.0 nM 5.14
CHEMBL45062 Ki = 10000.0 nM 5.00
CHEMBL44226 Ki = 11000.0 nM 4.96
CHEMBL43145 Ki = 14000.0 nM 4.85
CHEMBL44249 Ki = 20000.0 nM 4.70
CHEMBL296041 Ki = 20000.0 nM 4.70
CHEMBL42039 Ki = 23000.0 nM 4.64
CHEMBL44868 Ki = 23000.0 nM 4.64
CHEMBL42495 Ki = 29000.0 nM 4.54
CHEMBL42091 Ki = 100000.0 nM 4.00
CHEMBL42496 Ki > 100000.0 nM -