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Assay Detail

CHEMBL701580

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

Binding
Inhibitory activity against kallikrein
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 Expert

Target

Plasma kallikrein (CHEMBL2000)
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 9 6.41 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL174499 1 6.89
CHEMBL172360 1 6.68
CHEMBL175130 1 6.52
CHEMBL174558 1 6.42
CHEMBL176243 1 6.30
CHEMBL369086 1 6.30
CHEMBL367953 1 6.25
CHEMBL176671 1 6.19
CHEMBL369681 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL174499 IC50 = 130.0 nM 6.89
CHEMBL172360 IC50 = 210.0 nM 6.68
CHEMBL175130 IC50 = 300.0 nM 6.52
CHEMBL174558 IC50 = 380.0 nM 6.42
CHEMBL176243 IC50 = 500.0 nM 6.30
CHEMBL369086 IC50 = 500.0 nM 6.30
CHEMBL367953 IC50 = 560.0 nM 6.25
CHEMBL176671 IC50 = 640.0 nM 6.19
CHEMBL369681 IC50 = 790.0 nM 6.10