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Assay Detail

CHEMBL901117

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

Binding
Inhibition of bovine thrombin
14
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Prothrombin (CHEMBL4471)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Design and synthesis of novel and potent inhibitors of the type II transmembrane serine protease, matriptase, based upon the sunflower trypsin inhibitor-1.
Li P, Jiang S, Lee SL, Lin CY, Johnson MD, Dickson RB, Michejda CJ, Roller PP.
J Med Chem (2007) 50 : 5976 -5983
PubMed 17985858 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 4.90 6.07
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL394723 1 6.07
CHEMBL239127 1 5.30
CHEMBL409191 1 5.12
CHEMBL268861 1 5.00
CHEMBL240132 1 4.79
CHEMBL430087 1 4.59
CHEMBL410952 1 4.47
CHEMBL397831 1 4.39
CHEMBL267455 1 4.34
CHEMBL397832 1 -
CHEMBL394724 1 -
CHEMBL412487 1 -
CHEMBL412486 1 -
CHEMBL437180 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL394723 Ki = 860.0 nM 6.07
CHEMBL239127 Ki = 5000.0 nM 5.30
CHEMBL409191 Ki = 7630.0 nM 5.12
CHEMBL268861 Ki = 10000.0 nM 5.00
CHEMBL240132 Ki = 16300.0 nM 4.79
CHEMBL430087 Ki = 25600.0 nM 4.59
CHEMBL410952 Ki = 33600.0 nM 4.47
CHEMBL397831 Ki = 40400.0 nM 4.39
CHEMBL267455 Ki = 45600.0 nM 4.34
CHEMBL397832 Ki > 2500000.0 nM -
CHEMBL394724 Ki = 826800.0 nM -
CHEMBL412487 Ki = 163600.0 nM -
CHEMBL412486 Activity - -
CHEMBL437180 Ki - -