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Assay Detail

CHEMBL820677

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Binding
Inhibition of trypsin
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor.
Finch H, Pegg NA, McLaren J, Lowdon A, Bolton R, Coote SJ, Dyer U, Montana JG, Owen MR, Dowle M, Buckley D, Ross BC, Campbell C, Dix C, Mooney C, Man-Tang C, Patel C.
Bioorg Med Chem Lett (1998) 8 : 2955 -2960
PubMed 9873654 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 8.08 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL100989 1 10.70
CHEMBL99622 1 9.92
CHEMBL101041 1 9.30
CHEMBL101030 1 9.22
CHEMBL102081 1 8.70
CHEMBL102115 1 7.58
CHEMBL318001 1 7.48
CHEMBL323543 1 7.40
CHEMBL100672 1 7.39
CHEMBL457155 1 7.16
CHEMBL323544 1 6.66
CHEMBL102134 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL100989 IC50 = 0.02 nM 10.70
CHEMBL99622 IC50 = 0.12 nM 9.92
CHEMBL101041 IC50 = 0.5 nM 9.30
CHEMBL101030 IC50 = 0.6 nM 9.22
CHEMBL102081 IC50 = 2.0 nM 8.70
CHEMBL102115 IC50 = 26.0 nM 7.58
CHEMBL318001 IC50 = 33.0 nM 7.48
CHEMBL323543 IC50 = 40.0 nM 7.40
CHEMBL100672 IC50 = 41.0 nM 7.39
CHEMBL457155 IC50 = 70.0 nM 7.16
CHEMBL323544 IC50 = 220.0 nM 6.66
CHEMBL102134 IC50 = 3300.0 nM 5.48