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Assay Detail

CHEMBL659608

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

Binding
In vitro inhibitory activity against coagulation factor X.
51
Total Activities
51
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

Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity.
Zhang P, Bao L, Zuckett JF, Jia ZJ, Woolfrey J, Arfsten A, Edwards S, Sinha U, Hutchaleelaha A, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY.
Bioorg Med Chem Lett (2004) 14 : 989 -993
PubMed 15013007 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 8.09 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL367953 1 9.70
CHEMBL175130 1 9.52
CHEMBL369681 1 9.15
CHEMBL435741 1 9.10
CHEMBL174499 1 9.10
CHEMBL176243 1 9.05
CHEMBL176671 1 9.05
CHEMBL174558 1 9.00
CHEMBL174791 1 8.96
CHEMBL369023 1 8.89
CHEMBL368095 1 8.89
CHEMBL177444 1 8.85
CHEMBL172360 1 8.82
CHEMBL366358 1 8.82
CHEMBL355807 1 8.70
CHEMBL177109 1 8.70
CHEMBL426416 1 8.64
CHEMBL368494 1 8.46
CHEMBL369015 1 8.44
CHEMBL175033 1 8.42
CHEMBL369086 1 8.40
CHEMBL176210 1 8.30
CHEMBL173832 1 8.24
CHEMBL174731 1 8.20
CHEMBL175014 1 8.17
CHEMBL172256 1 8.16
CHEMBL425858 1 8.15
CHEMBL174968 1 8.00
CHEMBL176757 1 8.00
CHEMBL368126 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL367953 IC50 = 0.2 nM 9.70
CHEMBL175130 IC50 = 0.3 nM 9.52
CHEMBL369681 IC50 = 0.7 nM 9.15
CHEMBL435741 IC50 = 0.8 nM 9.10
CHEMBL174499 IC50 = 0.8 nM 9.10
CHEMBL176243 IC50 = 0.9 nM 9.05
CHEMBL176671 IC50 = 0.9 nM 9.05
CHEMBL174558 IC50 = 1.0 nM 9.00
CHEMBL174791 IC50 = 1.1 nM 8.96
CHEMBL369023 IC50 = 1.3 nM 8.89
CHEMBL368095 IC50 = 1.3 nM 8.89
CHEMBL177444 IC50 = 1.4 nM 8.85
CHEMBL172360 IC50 = 1.5 nM 8.82
CHEMBL366358 IC50 = 1.5 nM 8.82
CHEMBL177109 IC50 = 2.0 nM 8.70
CHEMBL355807 IC50 = 2.0 nM 8.70
CHEMBL426416 IC50 = 2.3 nM 8.64
CHEMBL368494 IC50 = 3.5 nM 8.46
CHEMBL369015 IC50 = 3.6 nM 8.44
CHEMBL175033 IC50 = 3.8 nM 8.42
CHEMBL369086 IC50 = 4.0 nM 8.40
CHEMBL176210 IC50 = 5.0 nM 8.30
CHEMBL173832 IC50 = 5.8 nM 8.24
CHEMBL174731 IC50 = 6.3 nM 8.20
CHEMBL175014 IC50 = 6.8 nM 8.17
CHEMBL172256 IC50 = 6.9 nM 8.16
CHEMBL425858 IC50 = 7.0 nM 8.15
CHEMBL174968 IC50 = 10.0 nM 8.00
CHEMBL176757 IC50 = 10.0 nM 8.00
CHEMBL368126 IC50 = 11.0 nM 7.96
CHEMBL369177 IC50 = 12.0 nM 7.92
CHEMBL368614 IC50 = 15.0 nM 7.82
CHEMBL176268 IC50 = 15.0 nM 7.82
CHEMBL367340 IC50 = 15.0 nM 7.82
CHEMBL425859 IC50 = 16.0 nM 7.80
CHEMBL175031 IC50 = 17.0 nM 7.77
CHEMBL175122 IC50 = 30.0 nM 7.52
CHEMBL368323 IC50 = 35.0 nM 7.46
CHEMBL174870 IC50 = 35.0 nM 7.46
CHEMBL368914 IC50 = 40.0 nM 7.40
CHEMBL176736 IC50 = 40.0 nM 7.40
CHEMBL176451 IC50 = 53.0 nM 7.28
CHEMBL366894 IC50 = 76.0 nM 7.12
CHEMBL176856 IC50 = 82.0 nM 7.09
CHEMBL174740 IC50 = 136.0 nM 6.87
CHEMBL368744 IC50 = 140.0 nM 6.85
CHEMBL175142 IC50 = 156.0 nM 6.81
CHEMBL366647 IC50 = 171.0 nM 6.77
CHEMBL175125 IC50 = 176.0 nM 6.75
CHEMBL174111 IC50 = 230.0 nM 6.64