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Assay Detail

CHEMBL761622

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

Binding
Inhibition of HRV Protease 3CP (serotype 14).
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human rhinovirus B
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Human rhinovirus A protease (CHEMBL2857)
Type SINGLE PROTEIN
Organism Human rhinovirus sp.

Publication

Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 6. Structure-activity studies of orally bioavailable, 2-pyridone-containing peptidomimetics.
Dragovich PS, Prins TJ, Zhou R, Brown EL, Maldonado FC, Fuhrman SA, Zalman LS, Tuntland T, Lee CA, Patick AK, Matthews DA, Hendrickson TF, Kosa MB, Liu B, Batugo MR, Gleeson JP, Sakata SK, Chen L, Guzman MC, Meador JW, Ferre RA, Worland ST.
J Med Chem (2002) 45 : 1607 -1623
PubMed 11931615 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 7.25 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL291277 1 9.00
CHEMBL289920 1 8.70
CHEMBL43972 1 8.52
CHEMBL44129 1 7.85
CHEMBL44567 1 7.80
CHEMBL44284 1 7.62
CHEMBL41437 1 7.47
CHEMBL29609 PLECONARIL 2.0 1 7.24
CHEMBL43385 1 6.98
CHEMBL40872 1 6.75
CHEMBL298019 PIRODAVIR 2.0 1 6.36
CHEMBL44022 1 6.33
CHEMBL42513 1 6.29
CHEMBL295096 1 6.05
CHEMBL44351 1 5.75
CHEMBL290485 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL291277 EC50 = 1.0 nM 9.00
CHEMBL289920 EC50 = 2.0 nM 8.70
CHEMBL43972 EC50 = 3.0 nM 8.52
CHEMBL44129 EC50 = 14.0 nM 7.85
CHEMBL44567 EC50 = 16.0 nM 7.80
CHEMBL44284 EC50 = 24.0 nM 7.62
CHEMBL41437 EC50 = 34.0 nM 7.47
CHEMBL29609 PLECONARIL EC50 = 58.0 nM 7.24
CHEMBL43385 EC50 = 104.0 nM 6.98
CHEMBL40872 EC50 = 178.0 nM 6.75
CHEMBL298019 PIRODAVIR EC50 = 440.0 nM 6.36
CHEMBL44022 EC50 = 469.0 nM 6.33
CHEMBL42513 EC50 = 518.0 nM 6.29
CHEMBL295096 EC50 = 888.0 nM 6.05
CHEMBL44351 EC50 = 1780.0 nM 5.75
CHEMBL290485 EC50 > 10000.0 nM -