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Assay Detail

CHEMBL828215

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

Binding
Binding affinity against bovine trypsin
66
Total Activities
65
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Serine protease 1 (CHEMBL3769)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design.
Costanzo MJ, Almond HR, Hecker LR, Schott MR, Yabut SC, Zhang HC, Andrade-Gordon P, Corcoran TW, Giardino EC, Kauffman JA, Lewis JM, de Garavilla L, Haertlein BJ, Maryanoff BE.
J Med Chem (2005) 48 : 1984 -2008
PubMed 15771442 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 66 7.62 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL179910 1 9.52
CHEMBL179245 1 9.52
CHEMBL322205 1 8.92
CHEMBL363003 1 8.92
CHEMBL427125 1 8.82
CHEMBL176063 1 8.82
CHEMBL366688 1 8.74
CHEMBL361822 1 8.74
CHEMBL360071 1 8.74
CHEMBL176031 1 8.70
CHEMBL366882 1 8.70
CHEMBL366653 1 8.62
CHEMBL179961 1 8.59
CHEMBL401737 1 8.57
CHEMBL176491 1 8.57
CHEMBL361379 1 8.54
CHEMBL176000 1 8.52
CHEMBL270437 1 8.51
CHEMBL176660 1 8.46
CHEMBL175497 1 8.43
CHEMBL368937 1 8.41
CHEMBL366902 1 8.41
CHEMBL369868 1 8.37
CHEMBL175620 1 8.36
CHEMBL179081 1 8.30
CHEMBL369008 1 8.28
CHEMBL175738 1 8.27
CHEMBL177769 1 8.22
CHEMBL366625 1 8.10
CHEMBL367647 1 8.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL179910 Ki = 0.3 nM 9.52
CHEMBL179245 Ki = 0.3 nM 9.52
CHEMBL363003 Ki = 1.2 nM 8.92
CHEMBL322205 Ki = 1.2 nM 8.92
CHEMBL427125 Ki = 1.5 nM 8.82
CHEMBL176063 Ki = 1.5 nM 8.82
CHEMBL366688 Ki = 1.8 nM 8.74
CHEMBL361822 Ki = 1.8 nM 8.74
CHEMBL360071 Ki = 1.8 nM 8.74
CHEMBL176031 Ki = 2.0 nM 8.70
CHEMBL366882 Ki = 2.0 nM 8.70
CHEMBL366653 Ki = 2.4 nM 8.62
CHEMBL179961 Ki = 2.6 nM 8.59
CHEMBL176491 Ki = 2.7 nM 8.57
CHEMBL401737 Ki = 2.7 nM 8.57
CHEMBL361379 Ki = 2.9 nM 8.54
CHEMBL176000 Ki = 3.0 nM 8.52
CHEMBL270437 Ki = 3.1 nM 8.51
CHEMBL176660 Ki = 3.5 nM 8.46
CHEMBL175497 Ki = 3.7 nM 8.43
CHEMBL368937 Ki = 3.9 nM 8.41
CHEMBL366902 Ki = 3.9 nM 8.41
CHEMBL369868 Ki = 4.3 nM 8.37
CHEMBL175620 Ki = 4.4 nM 8.36
CHEMBL179081 Ki = 5.0 nM 8.30
CHEMBL369008 Ki = 5.3 nM 8.28
CHEMBL175738 Ki = 5.4 nM 8.27
CHEMBL177769 Ki = 6.0 nM 8.22
CHEMBL366625 Ki = 8.0 nM 8.10
CHEMBL367647 Ki = 8.3 nM 8.08
CHEMBL273196 EFEGATRAN Ki = 9.1 nM 8.04
CHEMBL176348 Ki = 9.4 nM 8.03
CHEMBL360751 Ki = 9.3 nM 8.03
CHEMBL414655 Ki = 12.0 nM 7.92
CHEMBL175735 Ki = 13.0 nM 7.89
CHEMBL361377 Ki = 15.0 nM 7.82
CHEMBL257898 Ki = 16.0 nM 7.80
CHEMBL176161 Ki = 20.0 nM 7.70
CHEMBL368894 Ki = 22.0 nM 7.66
CHEMBL179210 Ki = 22.0 nM 7.66
CHEMBL175464 Ki = 26.0 nM 7.58
CHEMBL360684 Ki = 30.0 nM 7.52
CHEMBL367890 Ki = 31.0 nM 7.51
CHEMBL435514 Ki = 31.0 nM 7.51
CHEMBL3084979 Ki = 54.0 nM 7.27
CHEMBL360542 Ki = 57.0 nM 7.24
CHEMBL404728 Ki = 73.0 nM 7.14
CHEMBL367973 Ki = 87.0 nM 7.06
CHEMBL2096761 Ki = 210.0 nM 6.68
CHEMBL180219 Ki = 250.0 nM 6.60