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Assay Detail

CHEMBL691213

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

Functional
In vitro anti-rhinoviral activity against human rhinovirus serotypes 2,3,9,14,16,25 and 39
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Enterovirus
Confidence 1 — Organism
Curated By Expert

Target

Enterovirus (CHEMBL613749)
Type ORGANISM
Organism Enterovirus

Publication

Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 8. Pharmacological optimization of orally bioavailable 2-pyridone-containing peptidomimetics.
Dragovich PS, Prins TJ, Zhou R, Johnson TO, Hua Y, Luu HT, Sakata SK, Brown EL, Maldonado FC, Tuntland T, Lee CA, Fuhrman SA, Zalman LS, Patick AK, Matthews DA, Wu EY, Guo M, Borer BC, Nayyar NK, Moran T, Chen L, Rejto PA, Rose PW, Guzman MC, Dovalsantos EZ, Lee S, McGee K, Mohajeri M, Liese A, Tao J, Kosa MB, Liu B, Batugo MR, Gleeson JP, Wu ZP, Liu J, Meador JW, Ferre RA.
J Med Chem (2003) 46 : 4572 -4585
PubMed 14521419 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 6.92 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL291277 1 7.96
CHEMBL140521 1 7.44
CHEMBL141816 1 7.33
CHEMBL141157 IMOCITRELVIR 2.0 1 7.24
CHEMBL345023 1 7.19
CHEMBL140398 1 7.12
CHEMBL291276 1 7.11
CHEMBL140274 1 7.05
CHEMBL29609 PLECONARIL 2.0 1 6.87
CHEMBL141919 1 6.76
CHEMBL139662 1 6.56
CHEMBL336934 1 6.51
CHEMBL139782 1 6.44
CHEMBL139953 1 6.39
CHEMBL141136 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL291277 EC50 = 11.0 nM 7.96
CHEMBL140521 EC50 = 36.0 nM 7.44
CHEMBL141816 EC50 = 47.0 nM 7.33
CHEMBL141157 IMOCITRELVIR EC50 = 58.0 nM 7.24
CHEMBL345023 EC50 = 64.0 nM 7.19
CHEMBL140398 EC50 = 76.0 nM 7.12
CHEMBL291276 EC50 = 78.0 nM 7.11
CHEMBL140274 EC50 = 90.0 nM 7.05
CHEMBL29609 PLECONARIL EC50 = 136.0 nM 6.87
CHEMBL141919 EC50 = 174.0 nM 6.76
CHEMBL139662 EC50 = 276.0 nM 6.56
CHEMBL336934 EC50 = 310.0 nM 6.51
CHEMBL139782 EC50 = 361.0 nM 6.44
CHEMBL139953 EC50 = 405.0 nM 6.39
CHEMBL141136 EC50 = 1460.0 nM 5.84