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Assay Detail

CHEMBL1268155

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

Functional
Antiviral activity against HIV 1 NL4.3 integrase S230N mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MT4
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
Hombrouck A, Voet A, Van Remoortel B, Desadeleer C, De Maeyer M, Debyser Z, Witvrouw M.
Antimicrob Agents Chemother (2008) 52 : 2069 -2078
PubMed 18378713 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 7.81 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL204656 ELVITEGRAVIR 4.0 1 9.05
CHEMBL129 ZIDOVUDINE 4.0 1 8.22
CHEMBL414850 1 8.15
CHEMBL254316 RALTEGRAVIR 4.0 1 8.05
CHEMBL163 RITONAVIR 4.0 1 7.05
CHEMBL259011 1 6.31
CHEMBL18442 PLERIXAFOR 4.0 1 -
CHEMBL57 NEVIRAPINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL204656 ELVITEGRAVIR EC50 = 0.9 nM 9.05
CHEMBL129 ZIDOVUDINE EC50 = 6.0 nM 8.22
CHEMBL414850 EC50 = 7.0 nM 8.15
CHEMBL254316 RALTEGRAVIR EC50 = 9.0 nM 8.05
CHEMBL163 RITONAVIR EC50 = 90.0 nM 7.05
CHEMBL259011 EC50 = 490.0 nM 6.31
CHEMBL18442 PLERIXAFOR EC50 - -
CHEMBL57 NEVIRAPINE EC50 - -