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Assay Detail

CHEMBL4014630

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

Functional
Antiviral activity against HIV1 harboring Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Confidence 1 — Organism
Curated By Autocuration

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
Zhang H, Tian Y, Kang D, Huo Z, Zhou Z, Liu H, De Clercq E, Pannecouque C, Zhan P, Liu X.
Eur J Med Chem (2017) 130 : 209 -222
PubMed 28254696 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.26 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129 ZIDOVUDINE 4.0 1 7.96
CHEMBL308954 ETRAVIRINE 4.0 1 7.66
CHEMBL223228 EFAVIRENZ 4.0 1 6.47
CHEMBL929 DELAVIRDINE MESYLATE 4.0 1 6.16
CHEMBL57 NEVIRAPINE 4.0 1 5.02
CHEMBL4089736 1 4.28
CHEMBL4100493 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129 ZIDOVUDINE EC50 = 11.0 nM 7.96
CHEMBL308954 ETRAVIRINE EC50 = 22.0 nM 7.66
CHEMBL223228 EFAVIRENZ EC50 = 340.0 nM 6.47
CHEMBL929 DELAVIRDINE MESYLATE EC50 = 690.0 nM 6.16
CHEMBL57 NEVIRAPINE EC50 = 9610.0 nM 5.02
CHEMBL4089736 EC50 = 51950.0 nM 4.28
CHEMBL4100493 EC50 > 298000.0 nM -