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Assay Detail

CHEMBL968707

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

Binding
Inhibition of kallikrein
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 4 5.73 6.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL221906 1 6.29
CHEMBL472967 1 6.27
CHEMBL512351 BETRIXABAN 4.0 1 5.20
CHEMBL515919 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL221906 IC50 = 510.0 nM 6.29
CHEMBL472967 IC50 = 540.0 nM 6.27
CHEMBL512351 BETRIXABAN IC50 = 6300.0 nM 5.20
CHEMBL515919 IC50 = 7200.0 nM 5.14