Assay Detail

CHEMBL1640134

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

Functional

Selectivity ratio of EC50 for HIV1 8415-2 harboring reverse transcriptase 65R/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	8.62	8.92

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL515564	TENOFOVIR EXALIDEX	2.0	1	8.92
CHEMBL483	TENOFOVIR ANHYDROUS	3.0	1	8.48
CHEMBL129	ZIDOVUDINE	4.0	1	8.47

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL515564	TENOFOVIR EXALIDEX	EC50	=	1.2	nM	8.92
CHEMBL483	TENOFOVIR ANHYDROUS	EC50	=	3.3	nM	8.48
CHEMBL129	ZIDOVUDINE	EC50	=	3.4	nM	8.47