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Assay Detail

CHEMBL968695

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Binding
Inhibition of Factor 10a
ChEMBL ↗
67
Total Activities
62
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor.
Zhang P, Huang W, Wang L, Bao L, Jia ZJ, Bauer SM, Goldman EA, Probst GD, Song Y, Su T, Fan J, Wu Y, Li W, Woolfrey J, Sinha U, Wong PW, Edwards ST, Arfsten AE, Clizbe LA, Kanter J, Pandey A, Park G, Hutchaleelaha A, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY.
Bioorg Med Chem Lett (2009) 19 : 2179 -2185
PubMed 19297154 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 60 8.83 9.40
Ki 7 9.83 10.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL221906 — — 2 10.36
CHEMBL472967 — — 2 10.22
CHEMBL231779 APIXABAN 4.0 1 10.10
CHEMBL515919 — — 2 9.98
CHEMBL512351 BETRIXABAN 4.0 2 9.93
CHEMBL473771 — — 1 9.40
CHEMBL198362 RIVAROXABAN 4.0 1 9.40
CHEMBL515254 — — 1 9.30
CHEMBL475551 — — 1 9.30
CHEMBL513981 — — 1 9.30
CHEMBL472966 — — 1 9.30
CHEMBL472778 — — 1 9.30
CHEMBL515545 — — 1 9.22
CHEMBL472610 — — 1 9.22
CHEMBL221956 — — 1 9.15
CHEMBL475356 — — 1 9.15
CHEMBL471774 — — 1 9.15
CHEMBL470721 — — 1 9.15
CHEMBL513218 — — 1 9.10
CHEMBL515551 — — 1 9.05
CHEMBL473161 — — 1 9.05
CHEMBL470905 — — 1 9.05
CHEMBL218315 — — 1 9.05
CHEMBL475185 — — 1 9.00
CHEMBL471775 — — 1 9.00
CHEMBL475552 — — 1 9.00
CHEMBL470719 — — 1 8.96
CHEMBL471583 — — 1 8.96
CHEMBL516356 — — 1 8.92
CHEMBL516082 — — 1 8.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL221906 — Ki = 0.044 nM 10.36
CHEMBL472967 — Ki = 0.06 nM 10.22
CHEMBL231779 APIXABAN Ki = 0.08 nM 10.10
CHEMBL515919 — Ki = 0.105 nM 9.98
CHEMBL512351 BETRIXABAN Ki = 0.117 nM 9.93
CHEMBL473771 — IC50 = 0.4 nM 9.40
CHEMBL198362 RIVAROXABAN Ki = 0.4 nM 9.40
CHEMBL472778 — IC50 = 0.5 nM 9.30
CHEMBL472966 — IC50 = 0.5 nM 9.30
CHEMBL513981 — IC50 = 0.5 nM 9.30
CHEMBL475551 — IC50 = 0.5 nM 9.30
CHEMBL221906 — IC50 = 0.5 nM 9.30
CHEMBL515254 — IC50 = 0.5 nM 9.30
CHEMBL515545 — IC50 = 0.6 nM 9.22
CHEMBL472610 — IC50 = 0.6 nM 9.22
CHEMBL221956 — IC50 = 0.7 nM 9.15
CHEMBL515919 — IC50 = 0.7 nM 9.15
CHEMBL475356 — IC50 = 0.7 nM 9.15
CHEMBL470721 — IC50 = 0.7 nM 9.15
CHEMBL471774 — IC50 = 0.7 nM 9.15
CHEMBL513218 — IC50 = 0.8 nM 9.10
CHEMBL218315 — IC50 = 0.9 nM 9.05
CHEMBL515551 — IC50 = 0.9 nM 9.05
CHEMBL470905 — IC50 = 0.9 nM 9.05
CHEMBL473161 — IC50 = 0.9 nM 9.05
CHEMBL475552 — IC50 = 1.0 nM 9.00
CHEMBL471775 — IC50 = 1.0 nM 9.00
CHEMBL475185 — IC50 = 1.0 nM 9.00
CHEMBL470719 — IC50 = 1.1 nM 8.96
CHEMBL471583 — IC50 = 1.1 nM 8.96
CHEMBL472779 — IC50 = 1.2 nM 8.92
CHEMBL516356 — IC50 = 1.2 nM 8.92
CHEMBL472968 — IC50 = 1.2 nM 8.92
CHEMBL516082 — IC50 = 1.2 nM 8.92
CHEMBL473772 — IC50 = 1.3 nM 8.89
CHEMBL514616 — IC50 = 1.3 nM 8.89
CHEMBL471921 — IC50 = 1.3 nM 8.89
CHEMBL514667 — IC50 = 1.3 nM 8.89
CHEMBL471725 — Ki = 1.4 nM 8.85
CHEMBL511155 — IC50 = 1.4 nM 8.85
CHEMBL512351 BETRIXABAN IC50 = 1.5 nM 8.82
CHEMBL472599 — IC50 = 1.5 nM 8.82
CHEMBL473969 — IC50 = 1.5 nM 8.82
CHEMBL472609 — IC50 = 2.0 nM 8.70
CHEMBL219106 — IC50 = 2.0 nM 8.70
CHEMBL473359 — IC50 = 2.0 nM 8.70
CHEMBL470735 — IC50 = 2.0 nM 8.70
CHEMBL473571 — IC50 = 2.0 nM 8.70
CHEMBL514312 — IC50 = 2.0 nM 8.70
CHEMBL222012 — IC50 = 2.0 nM 8.70