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Assay Detail

CHEMBL3384577

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

Functional
Antiviral activity against wild type HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MT2
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
Lee WG, Frey KM, Gallardo-Macias R, Spasov KA, Bollini M, Anderson KS, Jorgensen WL.
ACS Med Chem Lett (2014) 5 : 1259 -1262
PubMed 25408842 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 33 6.91 9.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175691 RILPIVIRINE 4.0 1 9.19
CHEMBL3342986 1 8.28
CHEMBL3342991 1 8.25
CHEMBL308954 ETRAVIRINE 4.0 1 8.10
CHEMBL3342990 1 8.10
CHEMBL223228 EFAVIRENZ 4.0 1 8.00
CHEMBL3342988 1 8.00
CHEMBL3342985 1 7.89
CHEMBL1923492 1 7.80
CHEMBL3342984 1 7.72
CHEMBL3342992 1 7.50
CHEMBL3342966 1 7.34
CHEMBL3342989 1 7.32
CHEMBL1923490 1 7.31
CHEMBL3342987 1 7.31
CHEMBL3342979 1 6.80
CHEMBL3342976 1 6.77
CHEMBL3342975 1 6.66
CHEMBL3342978 1 6.60
CHEMBL3342974 1 6.51
CHEMBL3342983 1 6.37
CHEMBL3342977 1 6.22
CHEMBL3342982 1 6.00
CHEMBL3342971 1 5.72
CHEMBL3342972 1 5.46
CHEMBL3342980 1 5.24
CHEMBL3342981 1 4.92
CHEMBL3342969 1 4.57
CHEMBL3342967 1 4.42
CHEMBL3342970 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175691 RILPIVIRINE EC50 = 0.65 nM 9.19
CHEMBL3342986 EC50 = 5.3 nM 8.28
CHEMBL3342991 EC50 = 5.6 nM 8.25
CHEMBL308954 ETRAVIRINE EC50 = 8.0 nM 8.10
CHEMBL3342990 EC50 = 8.0 nM 8.10
CHEMBL223228 EFAVIRENZ EC50 = 10.0 nM 8.00
CHEMBL3342988 EC50 = 10.0 nM 8.00
CHEMBL3342985 EC50 = 13.0 nM 7.89
CHEMBL1923492 EC50 = 16.0 nM 7.80
CHEMBL3342984 EC50 = 19.0 nM 7.72
CHEMBL3342992 EC50 = 32.0 nM 7.50
CHEMBL3342966 EC50 = 46.0 nM 7.34
CHEMBL3342989 EC50 = 48.0 nM 7.32
CHEMBL1923490 EC50 = 49.0 nM 7.31
CHEMBL3342987 EC50 = 49.0 nM 7.31
CHEMBL3342979 EC50 = 160.0 nM 6.80
CHEMBL3342976 EC50 = 170.0 nM 6.77
CHEMBL3342975 EC50 = 220.0 nM 6.66
CHEMBL3342978 EC50 = 250.0 nM 6.60
CHEMBL3342974 EC50 = 310.0 nM 6.51
CHEMBL3342983 EC50 = 430.0 nM 6.37
CHEMBL3342977 EC50 = 600.0 nM 6.22
CHEMBL3342982 EC50 = 1000.0 nM 6.00
CHEMBL3342971 EC50 = 1900.0 nM 5.72
CHEMBL3342972 EC50 = 3500.0 nM 5.46
CHEMBL3342980 EC50 = 5700.0 nM 5.24
CHEMBL3342981 EC50 = 12000.0 nM 4.92
CHEMBL3342969 EC50 = 27000.0 nM 4.57
CHEMBL3342967 EC50 = 38000.0 nM 4.42
CHEMBL3342970 EC50 - -
CHEMBL3342968 EC50 - -
CHEMBL57 NEVIRAPINE EC50 - -
CHEMBL3342973 EC50 - -