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Assay Detail

CHEMBL4426070

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

Binding
Inhibition of human activated Protein C using Mes-DArg-Pro-Arg-AMC as substrate by Dixon plot analysis
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Vitamin K-dependent protein C (CHEMBL4444)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of Cyclic Plasmin Inhibitors: From Benzamidines to Benzylamines.
Hinkes S, Wuttke A, Saupe SM, Ivanova T, Wagner S, Knörlein A, Heine A, Klebe G, Steinmetzer T.
J Med Chem (2016) 59 : 6370 -6386
PubMed 27280436 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 4.38 5.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4591922 1 5.37
CHEMBL4458743 1 4.77
CHEMBL4441842 1 4.55
CHEMBL4437656 1 4.50
CHEMBL4466116 1 4.40
CHEMBL4577240 1 4.38
CHEMBL4545331 1 4.33
CHEMBL4444049 1 4.33
CHEMBL4443405 1 4.31
CHEMBL4515955 1 4.29
CHEMBL4476627 1 4.20
CHEMBL4466850 1 4.13
CHEMBL4583612 1 4.07
CHEMBL4458773 1 4.03
CHEMBL4519782 1 4.01
CHEMBL4553652 1 -
CHEMBL4560508 1 -
CHEMBL4441722 1 -
CHEMBL4472791 1 -
CHEMBL4454130 1 -
CHEMBL4476141 1 -
CHEMBL4571212 1 -
CHEMBL4549153 1 -
CHEMBL4547050 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4591922 Ki = 4280.0 nM 5.37
CHEMBL4458743 Ki = 17000.0 nM 4.77
CHEMBL4441842 Ki = 28017.0 nM 4.55
CHEMBL4437656 Ki = 32000.0 nM 4.50
CHEMBL4466116 Ki = 39740.0 nM 4.40
CHEMBL4577240 Ki = 42018.0 nM 4.38
CHEMBL4545331 Ki = 46500.0 nM 4.33
CHEMBL4444049 Ki = 47050.0 nM 4.33
CHEMBL4443405 Ki = 49340.0 nM 4.31
CHEMBL4515955 Ki = 51490.0 nM 4.29
CHEMBL4476627 Ki = 62910.0 nM 4.20
CHEMBL4466850 Ki = 74700.0 nM 4.13
CHEMBL4583612 Ki = 85870.0 nM 4.07
CHEMBL4458773 Ki = 93400.0 nM 4.03
CHEMBL4519782 Ki = 96500.0 nM 4.01
CHEMBL4553652 Ki > 100000.0 nM -
CHEMBL4560508 Ki > 100000.0 nM -
CHEMBL4441722 Ki = 130400.0 nM -
CHEMBL4472791 Ki > 100000.0 nM -
CHEMBL4454130 Ki > 30000.0 nM -
CHEMBL4476141 Ki > 13000.0 nM -
CHEMBL4571212 Ki > 30000.0 nM -
CHEMBL4549153 Ki = 212000.0 nM -
CHEMBL4547050 Ki = 106100.0 nM -