Assay Detail

CHEMBL1640129

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

Functional

Selectivity ratio of EC50 for HIV1 4755-5 harboring reverse transcriptase 41L/44D/67N/69D/118I/210W/215Y/184V mutant gene infected in human PBMC to EC50 for HIV1 NL 4-3 expressing wild type reverse transcriptase infected in human PBMC

ChEMBL ↗

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Target

Human immunodeficiency virus 1 (CHEMBL378) ↗

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Primary target Human immunodeficiency virus 1

CHEMBL378

Anchored from Assay target.

Protein identity Human immunodeficiency virus 1

Disease frame Disease evidence pending

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Total Activities

Compounds Tested

Activity Types

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

Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV.

Lanier ER, Ptak RG, Lampert BM, Keilholz L, Hartman T, Buckheit RW, Mankowski MK, Osterling MC, Almond MR, Painter GR.
Antimicrob Agents Chemother (2010) 54 : 2901 -2909
PubMed 20439609 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	3	7.72	8.68

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL515564	TENOFOVIR EXALIDEX	2.0	1	8.68
CHEMBL483	TENOFOVIR ANHYDROUS	3.0	1	7.75
CHEMBL129	ZIDOVUDINE	4.0	1	6.72

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL515564	TENOFOVIR EXALIDEX	EC50	=	2.1	nM	8.68
CHEMBL483	TENOFOVIR ANHYDROUS	EC50	=	18.0	nM	7.75
CHEMBL129	ZIDOVUDINE	EC50	=	190.0	nM	6.72