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Assay Detail

CHEMBL817281

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Binding
Compound was evaluated to inhibit the trypsin enzyme
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Serine protease 1 (CHEMBL209)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption.
Isaacs RC, Cutrona KJ, Newton CL, Sanderson PE, Solinsky MG, Baskin EP, Chen IW, Cooper CM, Cook JJ, Gardell SJ, Lewis SD, Lucas RJ, Lyle EA, Lynch JJ, Naylor-Olsen AM, Stranieri MT, Vastag K, Vacca JP.
Bioorg Med Chem Lett (1998) 8 : 1719 -1724
PubMed 9873422 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.52 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45480 1 5.85
CHEMBL431535 1 5.77
CHEMBL49457 1 5.72
CHEMBL46331 1 5.60
CHEMBL47920 1 5.58
CHEMBL11157 L-374087 1 5.50
CHEMBL46135 1 5.47
CHEMBL48929 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45480 Ki = 1400.0 nM 5.85
CHEMBL431535 Ki = 1700.0 nM 5.77
CHEMBL49457 Ki = 1900.0 nM 5.72
CHEMBL46331 Ki = 2500.0 nM 5.60
CHEMBL47920 Ki = 2600.0 nM 5.58
CHEMBL11157 L-374087 Ki = 3200.0 nM 5.50
CHEMBL46135 Ki = 3400.0 nM 5.47
CHEMBL48929 Ki = 20000.0 nM 4.70