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Assay Detail

CHEMBL968700

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Binding
Binding affinity to human ERG
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

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
Ki 9 6.29 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL221906 1 6.96
CHEMBL219106 1 6.70
CHEMBL472967 1 6.38
CHEMBL512351 BETRIXABAN 4.0 1 5.75
CHEMBL515919 1 5.68
CHEMBL474650 1 -
CHEMBL475370 1 -
CHEMBL221231 1 -
CHEMBL218315 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL221906 Ki = 110.0 nM 6.96
CHEMBL219106 Ki = 200.0 nM 6.70
CHEMBL472967 Ki = 420.0 nM 6.38
CHEMBL512351 BETRIXABAN Ki = 1800.0 nM 5.75
CHEMBL515919 Ki = 2100.0 nM 5.68
CHEMBL474650 Ki - -
CHEMBL475370 Ki - -
CHEMBL221231 Ki > 10000.0 nM -
CHEMBL218315 Ki > 10000.0 nM -