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Assay Detail

CHEMBL868541

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Binding
Inhibition of matriptase
56
Total Activities
56
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

Suppressor of tumorigenicity 14 protein (CHEMBL3018)
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 56 7.13 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL379068 1 8.82
CHEMBL378657 1 8.74
CHEMBL212014 1 8.41
CHEMBL378192 1 8.38
CHEMBL437307 1 8.30
CHEMBL379194 1 8.18
CHEMBL380221 1 8.06
CHEMBL3706846 1 7.89
CHEMBL378643 1 7.89
CHEMBL379586 1 7.85
CHEMBL3706845 1 7.68
CHEMBL211209 1 7.58
CHEMBL211401 1 7.55
CHEMBL209794 1 7.42
CHEMBL211659 1 7.38
CHEMBL379075 1 7.36
CHEMBL379357 1 7.35
CHEMBL210771 1 7.34
CHEMBL438959 1 7.30
CHEMBL3706847 1 7.28
CHEMBL380220 1 7.28
CHEMBL210244 1 7.24
CHEMBL212209 1 7.21
CHEMBL211367 1 7.21
CHEMBL209910 1 7.19
CHEMBL212310 1 7.14
CHEMBL212577 1 7.12
CHEMBL211811 1 7.09
CHEMBL211754 1 7.08
CHEMBL378830 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL379068 Ki = 1.5 nM 8.82
CHEMBL378657 Ki = 1.8 nM 8.74
CHEMBL212014 Ki = 3.9 nM 8.41
CHEMBL378192 Ki = 4.2 nM 8.38
CHEMBL437307 Ki = 5.0 nM 8.30
CHEMBL379194 Ki = 6.6 nM 8.18
CHEMBL380221 Ki = 8.7 nM 8.06
CHEMBL3706846 Ki = 13.0 nM 7.89
CHEMBL378643 Ki = 13.0 nM 7.89
CHEMBL379586 Ki = 14.0 nM 7.85
CHEMBL3706845 Ki = 21.0 nM 7.68
CHEMBL211209 Ki = 26.0 nM 7.58
CHEMBL211401 Ki = 28.0 nM 7.55
CHEMBL209794 Ki = 38.0 nM 7.42
CHEMBL211659 Ki = 42.0 nM 7.38
CHEMBL379075 Ki = 44.0 nM 7.36
CHEMBL379357 Ki = 45.0 nM 7.35
CHEMBL210771 Ki = 46.0 nM 7.34
CHEMBL438959 Ki = 50.0 nM 7.30
CHEMBL3706847 Ki = 53.0 nM 7.28
CHEMBL380220 Ki = 53.0 nM 7.28
CHEMBL210244 Ki = 57.0 nM 7.24
CHEMBL212209 Ki = 61.0 nM 7.21
CHEMBL211367 Ki = 61.0 nM 7.21
CHEMBL209910 Ki = 65.0 nM 7.19
CHEMBL212310 Ki = 72.0 nM 7.14
CHEMBL212577 Ki = 75.0 nM 7.12
CHEMBL211811 Ki = 82.0 nM 7.09
CHEMBL211754 Ki = 84.0 nM 7.08
CHEMBL378830 Ki = 88.0 nM 7.06
CHEMBL211086 Ki = 89.0 nM 7.05
CHEMBL377627 Ki = 89.0 nM 7.05
CHEMBL209963 Ki = 96.0 nM 7.02
CHEMBL212538 Ki = 100.0 nM 7.00
CHEMBL379186 Ki = 100.0 nM 7.00
CHEMBL211939 Ki = 110.0 nM 6.96
CHEMBL210189 Ki = 120.0 nM 6.92
CHEMBL208586 Ki = 130.0 nM 6.89
CHEMBL379960 Ki = 140.0 nM 6.85
CHEMBL212031 Ki = 140.0 nM 6.85
CHEMBL210815 Ki = 160.0 nM 6.80
CHEMBL212616 Ki = 170.0 nM 6.77
CHEMBL379957 Ki = 200.0 nM 6.70
CHEMBL212271 Ki = 210.0 nM 6.68
CHEMBL209586 Ki = 240.0 nM 6.62
CHEMBL379958 Ki = 250.0 nM 6.60
CHEMBL107955 Ki = 320.0 nM 6.50
CHEMBL210386 Ki = 330.0 nM 6.48
CHEMBL426501 Ki = 340.0 nM 6.47
CHEMBL377763 Ki = 380.0 nM 6.42