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Assay Detail

CHEMBL954314

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Binding
Inhibition of thrombin
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

Prothrombin (CHEMBL204)
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 5.60 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL493520 1 6.96
CHEMBL493117 1 6.57
CHEMBL445195 1 6.46
CHEMBL493140 1 6.40
CHEMBL498875 1 6.22
CHEMBL492342 1 6.17
CHEMBL444411 1 6.07
CHEMBL493116 1 5.90
CHEMBL507322 1 5.85
CHEMBL493936 1 5.68
CHEMBL494128 1 5.64
CHEMBL523865 1 5.29
CHEMBL378657 1 5.22
CHEMBL492334 1 4.97
CHEMBL495143 1 4.85
CHEMBL506479 1 4.84
CHEMBL492333 1 4.62
CHEMBL443990 1 4.54
CHEMBL493118 1 4.14
CHEMBL495010 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL493520 Ki = 110.0 nM 6.96
CHEMBL493117 Ki = 270.0 nM 6.57
CHEMBL445195 Ki = 350.0 nM 6.46
CHEMBL493140 Ki = 395.0 nM 6.40
CHEMBL498875 Ki = 600.0 nM 6.22
CHEMBL492342 Ki = 670.0 nM 6.17
CHEMBL444411 Ki = 850.0 nM 6.07
CHEMBL493116 Ki = 1250.0 nM 5.90
CHEMBL507322 Ki = 1400.0 nM 5.85
CHEMBL493936 Ki = 2100.0 nM 5.68
CHEMBL494128 Ki = 2300.0 nM 5.64
CHEMBL523865 Ki = 5100.0 nM 5.29
CHEMBL378657 Ki = 6000.0 nM 5.22
CHEMBL492334 Ki = 10600.0 nM 4.97
CHEMBL495143 Ki = 14000.0 nM 4.85
CHEMBL506479 Ki = 14500.0 nM 4.84
CHEMBL492333 Ki = 24200.0 nM 4.62
CHEMBL443990 Ki = 29000.0 nM 4.54
CHEMBL493118 Ki = 71700.0 nM 4.14
CHEMBL495010 Ki = 159000.0 nM -