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Assay Detail

CHEMBL812838

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Binding
Binding affinity towards thrombin was evaluated
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.
Sanderson PE, Cutrona KJ, Dorsey BD, Dyer DL, McDonough CM, Naylor-Olsen AM, Chen IW, Chen Z, Cook JJ, Gardell SJ, Krueger JA, Lewis SD, Lin JH, Lucas BJ, Lyle EA, Lynch JJ, Stranieri MT, Vastag K, Shafer JA, Vacca JP.
Bioorg Med Chem Lett (1998) 8 : 817 -822
PubMed 9871547 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.38 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL353431 1 9.48
CHEMBL287614 1 9.30
CHEMBL11157 L-374087 1 9.30
CHEMBL349430 1 8.64
CHEMBL355441 1 7.96
CHEMBL354555 1 7.92
CHEMBL96486 1 7.92
CHEMBL48929 1 7.58
CHEMBL424545 1 7.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL353431 Ki = 0.33 nM 9.48
CHEMBL287614 Ki = 0.5 nM 9.30
CHEMBL11157 L-374087 Ki = 0.5 nM 9.30
CHEMBL349430 Ki = 2.3 nM 8.64
CHEMBL355441 Ki = 11.0 nM 7.96
CHEMBL354555 Ki = 12.0 nM 7.92
CHEMBL96486 Ki = 12.0 nM 7.92
CHEMBL48929 Ki = 26.0 nM 7.58
CHEMBL424545 Ki = 47.0 nM 7.33