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Assay Detail

CHEMBL868544

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Binding
Inhibition of thrombin
ChEMBL ↗
54
Total Activities
54
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

Prothrombin (CHEMBL204) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptase.
Steinmetzer T, Schweinitz A, Stürzebecher A, Dönnecke D, Uhland K, Schuster O, Steinmetzer P, Müller F, Friedrich R, Than ME, Bode W, Stürzebecher J.
J Med Chem (2006) 49 : 4116 -4126
PubMed 16821772 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 54 5.88 7.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378830 — — 1 7.29
CHEMBL3706844 — — 1 7.27
CHEMBL378643 — — 1 7.00
CHEMBL210771 — — 1 6.96
CHEMBL211086 — — 1 6.92
CHEMBL209586 — — 1 6.77
CHEMBL211659 — — 1 6.77
CHEMBL212310 — — 1 6.72
CHEMBL209841 — — 1 6.70
CHEMBL211939 — — 1 6.68
CHEMBL209794 — — 1 6.68
CHEMBL379957 — — 1 6.58
CHEMBL380220 — — 1 6.57
CHEMBL377627 — — 1 6.52
CHEMBL3706845 — — 1 6.38
CHEMBL3706846 — — 1 6.38
CHEMBL379075 — — 1 6.34
CHEMBL107955 — — 1 6.31
CHEMBL209963 — — 1 6.31
CHEMBL379958 — — 1 6.24
CHEMBL210815 — — 1 6.22
CHEMBL209910 — — 1 6.21
CHEMBL210386 — — 1 5.92
CHEMBL212538 — — 1 5.89
CHEMBL211367 — — 1 5.89
CHEMBL212271 — — 1 5.85
CHEMBL211549 — — 1 5.82
CHEMBL210244 — — 1 5.80
CHEMBL211209 — — 1 5.77
CHEMBL3706847 — — 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378830 — Ki = 51.0 nM 7.29
CHEMBL3706844 — Ki = 54.0 nM 7.27
CHEMBL378643 — Ki = 99.0 nM 7.00
CHEMBL210771 — Ki = 110.0 nM 6.96
CHEMBL211086 — Ki = 120.0 nM 6.92
CHEMBL209586 — Ki = 170.0 nM 6.77
CHEMBL211659 — Ki = 170.0 nM 6.77
CHEMBL212310 — Ki = 190.0 nM 6.72
CHEMBL209841 — Ki = 200.0 nM 6.70
CHEMBL211939 — Ki = 210.0 nM 6.68
CHEMBL209794 — Ki = 210.0 nM 6.68
CHEMBL379957 — Ki = 260.0 nM 6.58
CHEMBL380220 — Ki = 270.0 nM 6.57
CHEMBL377627 — Ki = 300.0 nM 6.52
CHEMBL3706846 — Ki = 420.0 nM 6.38
CHEMBL3706845 — Ki = 420.0 nM 6.38
CHEMBL379075 — Ki = 460.0 nM 6.34
CHEMBL107955 — Ki = 490.0 nM 6.31
CHEMBL209963 — Ki = 490.0 nM 6.31
CHEMBL379958 — Ki = 580.0 nM 6.24
CHEMBL210815 — Ki = 600.0 nM 6.22
CHEMBL209910 — Ki = 620.0 nM 6.21
CHEMBL210386 — Ki = 1200.0 nM 5.92
CHEMBL212538 — Ki = 1300.0 nM 5.89
CHEMBL211367 — Ki = 1300.0 nM 5.89
CHEMBL212271 — Ki = 1400.0 nM 5.85
CHEMBL211549 — Ki = 1500.0 nM 5.82
CHEMBL210244 — Ki = 1600.0 nM 5.80
CHEMBL211209 — Ki = 1700.0 nM 5.77
CHEMBL3706847 — Ki = 1800.0 nM 5.75
CHEMBL379357 — Ki = 1800.0 nM 5.75
CHEMBL380221 — Ki = 1800.0 nM 5.75
CHEMBL426501 — Ki = 2500.0 nM 5.60
CHEMBL438959 — Ki = 2500.0 nM 5.60
CHEMBL209334 — Ki = 2600.0 nM 5.58
CHEMBL211794 — Ki = 3000.0 nM 5.52
CHEMBL212616 — Ki = 3300.0 nM 5.48
CHEMBL378192 — Ki = 4000.0 nM 5.40
CHEMBL379068 — Ki = 4000.0 nM 5.40
CHEMBL212209 — Ki = 4200.0 nM 5.38
CHEMBL208586 — Ki = 5000.0 nM 5.30
CHEMBL379586 — Ki = 5000.0 nM 5.30
CHEMBL379186 — Ki = 5400.0 nM 5.27
CHEMBL378657 — Ki = 6000.0 nM 5.22
CHEMBL212577 — Ki = 7000.0 nM 5.16
CHEMBL211401 — Ki = 8800.0 nM 5.06
CHEMBL379960 — Ki = 9400.0 nM 5.03
CHEMBL210189 — Ki = 12000.0 nM 4.92
CHEMBL211754 — Ki = 13000.0 nM 4.89
CHEMBL437307 — Ki = 13000.0 nM 4.89