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Assay Detail

CHEMBL995173

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Binding
Inhibition of human trypsin by Dixon-plot method
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Trypsin (CHEMBL2095204)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Orally active factor Xa inhibitors: investigation of a novel series of 3-amidinophenylsulfonamide derivatives using an amidoxime prodrug strategy.
Uchida M, Okazaki K, Mukaiyama H, Isawa H, Kobayashi H, Shiohara H, Muranaka H, Kai Y, Kikuchi N, Takeuchi H, Yokoyama K, Tsuji E, Ozawa T, Hoyano Y, Koizumi T, Misawa K, Hara K, Nakano S, Murakami Y, Okuno H.
Bioorg Med Chem Lett (2008) 18 : 4682 -4687
PubMed 18667303 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.75 6.11
IC50 2 5.39 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL455914 1 6.11
CHEMBL463581 1 6.10
CHEMBL463179 1 5.93
CHEMBL513605 1 5.77
CHEMBL457391 1 5.40
CHEMBL463385 1 5.21
CHEMBL513433 1 5.01
CHEMBL457392 1 -
CHEMBL456763 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL455914 Ki = 770.0 nM 6.11
CHEMBL463581 Ki = 800.0 nM 6.10
CHEMBL463179 Ki = 1170.0 nM 5.93
CHEMBL513605 IC50 = 1700.0 nM 5.77
CHEMBL457391 Ki = 4000.0 nM 5.40
CHEMBL463385 Ki = 6170.0 nM 5.21
CHEMBL513433 IC50 = 9700.0 nM 5.01
CHEMBL457392 Ki - -
CHEMBL456763 Ki - -