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Assay Detail

CHEMBL830302

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Binding
Inhibitory activity against coagulation factor Xa
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Coagulation factor X (CHEMBL244)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents.
Nazaré M, Essrich M, Will DW, Matter H, Ritter K, Urmann M, Bauer A, Schreuder H, Dudda A, Czech J, Lorenz M, Laux V, Wehner V.
Bioorg Med Chem Lett (2004) 14 : 4191 -4195
PubMed 15261268 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 6.87 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL182597 1 9.00
CHEMBL368238 1 8.52
CHEMBL184988 1 8.52
CHEMBL182746 1 8.52
CHEMBL182577 1 8.40
CHEMBL182755 1 7.82
CHEMBL181849 1 7.40
CHEMBL361147 1 7.24
CHEMBL181533 1 7.14
CHEMBL182323 1 7.05
CHEMBL182562 1 6.54
CHEMBL362810 1 6.40
CHEMBL363262 1 6.32
CHEMBL359721 1 6.18
CHEMBL181694 1 6.09
CHEMBL362052 1 5.68
CHEMBL360510 1 5.65
CHEMBL180080 1 5.61
CHEMBL182987 1 5.60
CHEMBL363485 1 5.56
CHEMBL360477 1 5.04
CHEMBL182845 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL182597 Ki = 1.0 nM 9.00
CHEMBL368238 Ki = 3.0 nM 8.52
CHEMBL184988 Ki = 3.0 nM 8.52
CHEMBL182746 Ki = 3.0 nM 8.52
CHEMBL182577 Ki = 4.0 nM 8.40
CHEMBL182755 Ki = 15.0 nM 7.82
CHEMBL181849 Ki = 40.0 nM 7.40
CHEMBL361147 Ki = 57.0 nM 7.24
CHEMBL181533 Ki = 73.0 nM 7.14
CHEMBL182323 Ki = 89.0 nM 7.05
CHEMBL182562 Ki = 287.0 nM 6.54
CHEMBL362810 Ki = 400.0 nM 6.40
CHEMBL363262 Ki = 474.0 nM 6.32
CHEMBL359721 Ki = 654.0 nM 6.18
CHEMBL181694 Ki = 810.0 nM 6.09
CHEMBL362052 Ki = 2100.0 nM 5.68
CHEMBL360510 Ki = 2230.0 nM 5.65
CHEMBL180080 Ki = 2480.0 nM 5.61
CHEMBL182987 Ki = 2500.0 nM 5.60
CHEMBL363485 Ki = 2730.0 nM 5.56
CHEMBL360477 Ki = 9010.0 nM 5.04
CHEMBL182845 Ki > 10000.0 nM -