Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL771785

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

Binding
In vitro inhibition of human thrombin catalytic activity after 3 min pre incubation.
21
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thrombin active site inhibitors: chemical synthesis, in vitro and in vivo pharmacological profile of a novel and selective agent BMS-189090 and analogues.
Das J, Kimball SD, Reid JA, Wang TC, Lau WF, Roberts DG, Seiler SM, Schumacher WA, Ogletree ML.
Bioorg Med Chem Lett (2002) 12 : 41 -44
PubMed 11738569 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.54 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL136198 1 7.92
CHEMBL423723 1 7.89
CHEMBL138877 2 7.80
CHEMBL337372 1 7.50
CHEMBL138935 1 7.30
CHEMBL421919 1 7.12
CHEMBL139207 1 7.10
CHEMBL136755 1 6.96
CHEMBL343953 1 6.70
CHEMBL342904 1 6.51
CHEMBL138783 1 6.41
CHEMBL424479 1 6.30
CHEMBL134916 1 6.21
CHEMBL136876 1 6.19
CHEMBL136076 1 5.85
CHEMBL136216 1 5.77
CHEMBL136082 1 5.55
CHEMBL344825 1 5.13
CHEMBL344239 1 4.85
CHEMBL137562 1 4.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL136198 IC50 = 12.0 nM 7.92
CHEMBL423723 IC50 = 13.0 nM 7.89
CHEMBL138877 IC50 = 16.0 nM 7.80
CHEMBL138877 IC50 = 18.0 nM 7.75
CHEMBL337372 IC50 = 32.0 nM 7.50
CHEMBL138935 IC50 = 50.0 nM 7.30
CHEMBL421919 IC50 = 75.0 nM 7.12
CHEMBL139207 IC50 = 80.0 nM 7.10
CHEMBL136755 IC50 = 110.0 nM 6.96
CHEMBL343953 IC50 = 200.0 nM 6.70
CHEMBL342904 IC50 = 310.0 nM 6.51
CHEMBL138783 IC50 = 390.0 nM 6.41
CHEMBL424479 IC50 = 500.0 nM 6.30
CHEMBL134916 IC50 = 620.0 nM 6.21
CHEMBL136876 IC50 = 650.0 nM 6.19
CHEMBL136076 IC50 = 1400.0 nM 5.85
CHEMBL136216 IC50 = 1700.0 nM 5.77
CHEMBL136082 IC50 = 2800.0 nM 5.55
CHEMBL344825 IC50 = 7400.0 nM 5.13
CHEMBL344239 IC50 = 14000.0 nM 4.85
CHEMBL137562 IC50 = 27000.0 nM 4.57