Assay Detail

CHEMBL5119167

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

Functional

Antiviral activity against HIV1 wild type subtype B NL (4 to 3) harbouring V362/Q369/V370/T371 transfected in human HEK293T cells by dual-luciferase reporter assay

ChEMBL ↗

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Target

Human immunodeficiency virus 1 (CHEMBL378) ↗

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Human immunodeficiency virus 1 (CHEMBL378) is the working anchor for this assay review. Loading the live Open DB target snapshot…

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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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Functional
Organism	Human immunodeficiency virus 1
Cell Type	HEK293T
Confidence	1 — Organism
Curated By	Autocuration

Target

Human immunodeficiency virus 1 (CHEMBL378) ↗

Type	ORGANISM
Organism	Human immunodeficiency virus 1

Publication

The Discovery of GSK3640254, a Next-Generation Inhibitor of HIV-1 Maturation.

Regueiro-Ren A, Sit SY, Chen Y, Chen J, Swidorski JJ, Liu Z, Venables BL, Sin N, Hartz RA, Protack T, Lin Z, Zhang S, Li Z, Wu DR, Li P, Kempson J, Hou X, Gupta A, Rampulla R, Mathur A, Park H, Sarjeant A, Benitex Y, Rahematpura S, Parker D, Phillips T, Haskell R, Jenkins S, Santone KS, Cockett M, Hanumegowda U, Dicker I, Meanwell NA, Krystal M.
J Med Chem (2022) 65 : 11927 -11948
PubMed 36044257 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	2	8.76	8.96

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL5201510	FIPRAVIRIMAT	2.0	1	8.96
CHEMBL3827379	BMS-955176	2.0	1	8.55

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL5201510	FIPRAVIRIMAT	EC50	=	1.1	nM	8.96
CHEMBL3827379	BMS-955176	EC50	=	2.8	nM	8.55