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Assay Detail

CHEMBL659607

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Binding
In vitro inhibitory activity against human coagulation factor X
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.
Jia ZJ, Wu Y, Huang W, Zhang P, Song Y, Woolfrey J, Sinha U, Arfsten AE, Edwards ST, Hutchaleelaha A, Hollennbach SJ, Lambing JL, Scarborough RM, Zhu BY.
Bioorg Med Chem Lett (2004) 14 : 1229 -1234
PubMed 14980671 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 7.68 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20438 1 9.00
CHEMBL281838 1 8.70
CHEMBL281141 1 8.70
CHEMBL21250 1 8.70
CHEMBL279486 1 8.52
CHEMBL277657 1 8.40
CHEMBL20918 1 8.30
CHEMBL21179 1 8.22
CHEMBL20932 1 8.15
CHEMBL20496 1 8.15
CHEMBL20390 1 8.15
CHEMBL21562 1 8.10
CHEMBL20897 1 8.10
CHEMBL20391 1 8.10
CHEMBL2092985 1 8.00
CHEMBL282676 1 7.96
CHEMBL20488 1 7.92
CHEMBL280925 1 7.85
CHEMBL418558 1 7.82
CHEMBL281186 1 7.82
CHEMBL417826 1 7.80
CHEMBL277943 1 7.75
CHEMBL21052 1 7.75
CHEMBL21140 1 7.66
CHEMBL21506 1 7.66
CHEMBL282945 1 7.62
CHEMBL281801 1 7.55
CHEMBL431693 1 7.51
CHEMBL21176 1 7.47
CHEMBL418559 1 7.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20438 IC50 = 1.0 nM 9.00
CHEMBL281838 IC50 = 2.0 nM 8.70
CHEMBL21250 IC50 = 2.0 nM 8.70
CHEMBL281141 IC50 = 2.0 nM 8.70
CHEMBL279486 IC50 = 3.0 nM 8.52
CHEMBL277657 IC50 = 4.0 nM 8.40
CHEMBL20918 IC50 = 5.0 nM 8.30
CHEMBL21179 IC50 = 6.0 nM 8.22
CHEMBL20932 IC50 = 7.0 nM 8.15
CHEMBL20496 IC50 = 7.0 nM 8.15
CHEMBL20390 IC50 = 7.0 nM 8.15
CHEMBL20897 IC50 = 8.0 nM 8.10
CHEMBL20391 IC50 = 8.0 nM 8.10
CHEMBL21562 IC50 = 8.0 nM 8.10
CHEMBL2092985 IC50 = 10.0 nM 8.00
CHEMBL282676 IC50 = 11.0 nM 7.96
CHEMBL20488 IC50 = 12.0 nM 7.92
CHEMBL280925 IC50 = 14.0 nM 7.85
CHEMBL418558 IC50 = 15.0 nM 7.82
CHEMBL281186 IC50 = 15.0 nM 7.82
CHEMBL417826 IC50 = 16.0 nM 7.80
CHEMBL277943 IC50 = 18.0 nM 7.75
CHEMBL21052 IC50 = 18.0 nM 7.75
CHEMBL21140 IC50 = 22.0 nM 7.66
CHEMBL21506 IC50 = 22.0 nM 7.66
CHEMBL282945 IC50 = 24.0 nM 7.62
CHEMBL281801 IC50 = 28.0 nM 7.55
CHEMBL431693 IC50 = 31.0 nM 7.51
CHEMBL21176 IC50 = 34.0 nM 7.47
CHEMBL418559 IC50 = 48.0 nM 7.32
CHEMBL278141 IC50 = 50.0 nM 7.30
CHEMBL428530 IC50 = 50.0 nM 7.30
CHEMBL416181 IC50 = 76.0 nM 7.12
CHEMBL280336 IC50 = 80.0 nM 7.10
CHEMBL20567 IC50 = 110.0 nM 6.96
CHEMBL20673 IC50 = 110.0 nM 6.96
CHEMBL20420 IC50 = 114.0 nM 6.94
CHEMBL282703 IC50 = 134.0 nM 6.87
CHEMBL280214 IC50 = 377.0 nM 6.42
CHEMBL279487 IC50 = 479.0 nM 6.32
CHEMBL20651 IC50 = 511.0 nM 6.29
CHEMBL20396 IC50 = 777.0 nM 6.11