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Assay Detail

CHEMBL818172

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

Binding
Inhibitory concentration required against trypsin was determined
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 2.
Cody WL, Augelli-Szafran CE, Berryman KA, Cai C, Doherty AM, Edmunds JJ, He JX, Narasimhan LS, Penvose-Yi J, Plummer JS, Rapundalo ST, Rubin JR, Van Huis CA, Leblond L, Winocour PD, Siddiqui MA.
Bioorg Med Chem Lett (1999) 9 : 2503 -2508
PubMed 10498197 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.17 7.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL313790 1 7.02
CHEMBL256219 1 6.47
CHEMBL310722 1 5.64
CHEMBL83001 1 5.43
CHEMBL433144 1 5.39
CHEMBL84084 1 5.32
CHEMBL315086 1 5.32
CHEMBL314462 1 5.16
CHEMBL312904 1 5.14
CHEMBL313769 1 5.11
CHEMBL80013 1 5.07
CHEMBL82753 1 5.06
CHEMBL404654 1 5.04
CHEMBL312151 1 5.04
CHEMBL83260 1 5.01
CHEMBL79245 1 4.96
CHEMBL84536 1 4.85
CHEMBL309298 1 4.82
CHEMBL83692 1 4.77
CHEMBL408553 1 4.74
CHEMBL84083 1 4.68
CHEMBL420589 1 4.60
CHEMBL314791 1 4.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL313790 IC50 = 96.0 nM 7.02
CHEMBL256219 IC50 = 340.0 nM 6.47
CHEMBL310722 IC50 = 2300.0 nM 5.64
CHEMBL83001 IC50 = 3700.0 nM 5.43
CHEMBL433144 IC50 = 4100.0 nM 5.39
CHEMBL84084 IC50 = 4800.0 nM 5.32
CHEMBL315086 IC50 = 4800.0 nM 5.32
CHEMBL314462 IC50 = 7000.0 nM 5.16
CHEMBL312904 IC50 = 7200.0 nM 5.14
CHEMBL313769 IC50 = 7800.0 nM 5.11
CHEMBL80013 IC50 = 8500.0 nM 5.07
CHEMBL82753 IC50 = 8700.0 nM 5.06
CHEMBL404654 IC50 = 9100.0 nM 5.04
CHEMBL312151 IC50 = 9100.0 nM 5.04
CHEMBL83260 IC50 = 9700.0 nM 5.01
CHEMBL79245 IC50 = 11000.0 nM 4.96
CHEMBL84536 IC50 = 14000.0 nM 4.85
CHEMBL309298 IC50 = 15000.0 nM 4.82
CHEMBL83692 IC50 = 17000.0 nM 4.77
CHEMBL408553 IC50 = 18200.0 nM 4.74
CHEMBL84083 IC50 = 21000.0 nM 4.68
CHEMBL420589 IC50 = 25000.0 nM 4.60
CHEMBL314791 IC50 = 45000.0 nM 4.35