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Assay Detail

CHEMBL817818

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

Binding
Inhibitory activity against trypsin was determined
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

Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates.
Sanderson PE, Lyle TA, Cutrona KJ, Dyer DL, Dorsey BD, McDonough CM, Naylor-Olsen AM, Chen IW, Chen Z, Cook JJ, Cooper CM, Gardell SJ, Hare TR, Krueger JA, Lewis SD, Lin JH, Lucas BJ, Lyle EA, Lynch JJ, Stranieri MT, Vastag K, Yan Y, Shafer JA, Vacca JP.
J Med Chem (1998) 41 : 4466 -4474
PubMed 9804686 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.70 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL138855 1 6.00
CHEMBL139331 1 5.92
CHEMBL336438 1 5.82
CHEMBL19080 L-375378 1 5.75
CHEMBL140885 1 5.68
CHEMBL141266 1 5.58
CHEMBL11157 L-374087 1 5.50
CHEMBL139178 1 5.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL138855 Ki = 1000.0 nM 6.00
CHEMBL139331 Ki = 1200.0 nM 5.92
CHEMBL336438 Ki = 1500.0 nM 5.82
CHEMBL19080 L-375378 Ki = 1800.0 nM 5.75
CHEMBL140885 Ki = 2100.0 nM 5.68
CHEMBL141266 Ki = 2600.0 nM 5.58
CHEMBL11157 L-374087 Ki = 3200.0 nM 5.50
CHEMBL139178 Ki = 4800.0 nM 5.32