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Assay Detail

CHEMBL813635

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

Binding
Binding affinity towards thrombin obtained from human purified enzymes
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2.
Quan ML, Ellis CD, Liauw AY, Alexander RS, Knabb RM, Lam G, Wright MR, Wong PC, Wexler RR.
J Med Chem (1999) 42 : 2760 -2773
PubMed 10425087 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 40 5.59 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL264626 1 7.16
CHEMBL321530 1 7.00
CHEMBL323309 1 6.52
CHEMBL329460 1 6.52
CHEMBL159418 1 6.40
CHEMBL323310 1 6.30
CHEMBL7651 1 6.05
CHEMBL328069 1 6.05
CHEMBL93210 1 5.96
CHEMBL316070 1 5.89
CHEMBL406295 1 5.70
CHEMBL1184021 1 5.68
CHEMBL328298 1 5.62
CHEMBL327201 1 5.55
CHEMBL91999 1 5.54
CHEMBL1183989 1 5.52
CHEMBL279628 1 5.51
CHEMBL328582 1 5.51
CHEMBL436684 1 5.47
CHEMBL328451 1 5.41
CHEMBL327404 1 5.41
CHEMBL92523 1 5.41
CHEMBL330284 1 5.40
CHEMBL327403 1 5.37
CHEMBL94052 1 5.36
CHEMBL327473 1 5.35
CHEMBL1183796 1 5.30
CHEMBL330496 1 5.24
CHEMBL93744 1 5.24
CHEMBL445678 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL264626 Ki = 70.0 nM 7.16
CHEMBL321530 Ki = 100.0 nM 7.00
CHEMBL329460 Ki = 300.0 nM 6.52
CHEMBL323309 Ki = 300.0 nM 6.52
CHEMBL159418 Ki = 400.0 nM 6.40
CHEMBL323310 Ki = 500.0 nM 6.30
CHEMBL7651 Ki = 900.0 nM 6.05
CHEMBL328069 Ki = 900.0 nM 6.05
CHEMBL93210 Ki = 1100.0 nM 5.96
CHEMBL316070 Ki = 1300.0 nM 5.89
CHEMBL406295 Ki = 2000.0 nM 5.70
CHEMBL1184021 Ki = 2100.0 nM 5.68
CHEMBL328298 Ki = 2400.0 nM 5.62
CHEMBL327201 Ki = 2800.0 nM 5.55
CHEMBL91999 Ki = 2900.0 nM 5.54
CHEMBL1183989 Ki = 3000.0 nM 5.52
CHEMBL279628 Ki = 3100.0 nM 5.51
CHEMBL328582 Ki = 3100.0 nM 5.51
CHEMBL436684 Ki = 3400.0 nM 5.47
CHEMBL92523 Ki = 3900.0 nM 5.41
CHEMBL327404 Ki = 3900.0 nM 5.41
CHEMBL328451 Ki = 3900.0 nM 5.41
CHEMBL330284 Ki = 4000.0 nM 5.40
CHEMBL327403 Ki = 4300.0 nM 5.37
CHEMBL94052 Ki = 4400.0 nM 5.36
CHEMBL327473 Ki = 4500.0 nM 5.35
CHEMBL1183796 Ki = 5000.0 nM 5.30
CHEMBL330496 Ki = 5800.0 nM 5.24
CHEMBL93744 Ki = 5800.0 nM 5.24
CHEMBL445678 Ki = 6100.0 nM 5.21
CHEMBL92909 Ki = 7400.0 nM 5.13
CHEMBL327331 Ki = 7700.0 nM 5.11
CHEMBL92609 Ki = 8100.0 nM 5.09
CHEMBL318112 Ki = 8400.0 nM 5.08
CHEMBL316311 Ki = 10000.0 nM 5.00
CHEMBL328805 Ki = 13000.0 nM 4.89
CHEMBL327213 Ki = 14000.0 nM 4.85
CHEMBL327405 Ki = 16000.0 nM 4.80
CHEMBL316318 Ki > 21000.0 nM -
CHEMBL328577 Ki > 21000.0 nM -