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Assay Detail

CHEMBL954312

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Binding
Inhibition of matriptase
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Suppressor of tumorigenicity 14 protein (CHEMBL3018)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Incorporation of neutral C-terminal residues in 3-amidinophenylalanine-derived matriptase inhibitors.
Schweinitz A, Dönnecke D, Ludwig A, Steinmetzer P, Schulze A, Kotthaus J, Wein S, Clement B, Steinmetzer T.
Bioorg Med Chem Lett (2009) 19 : 1960 -1965
PubMed 19250826 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.25 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378657 1 8.74
CHEMBL498875 1 8.21
CHEMBL444411 1 8.20
CHEMBL507322 1 8.12
CHEMBL492342 1 7.92
CHEMBL493116 1 7.89
CHEMBL445195 1 7.77
CHEMBL493936 1 7.51
CHEMBL493117 1 7.48
CHEMBL493118 1 7.43
CHEMBL493520 1 7.28
CHEMBL443990 1 7.28
CHEMBL523865 1 7.19
CHEMBL492333 1 7.00
CHEMBL506479 1 6.82
CHEMBL494128 1 6.75
CHEMBL495143 1 6.59
CHEMBL493140 1 6.33
CHEMBL492334 1 5.62
CHEMBL495010 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378657 Ki = 1.8 nM 8.74
CHEMBL498875 Ki = 6.1 nM 8.21
CHEMBL444411 Ki = 6.3 nM 8.20
CHEMBL507322 Ki = 7.5 nM 8.12
CHEMBL492342 Ki = 12.0 nM 7.92
CHEMBL493116 Ki = 13.0 nM 7.89
CHEMBL445195 Ki = 17.0 nM 7.77
CHEMBL493936 Ki = 31.0 nM 7.51
CHEMBL493117 Ki = 33.0 nM 7.48
CHEMBL493118 Ki = 37.0 nM 7.43
CHEMBL493520 Ki = 53.0 nM 7.28
CHEMBL443990 Ki = 53.0 nM 7.28
CHEMBL523865 Ki = 65.0 nM 7.19
CHEMBL492333 Ki = 100.0 nM 7.00
CHEMBL506479 Ki = 150.0 nM 6.82
CHEMBL494128 Ki = 180.0 nM 6.75
CHEMBL495143 Ki = 255.0 nM 6.59
CHEMBL493140 Ki = 470.0 nM 6.33
CHEMBL492334 Ki = 2400.0 nM 5.62
CHEMBL495010 Ki = 11000.0 nM 4.96