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Assay Detail

CHEMBL691412

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

Binding
Inhibitory concentration against Recombinant HIV-1 integrase (Standard transfer reaction)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Human immunodeficiency virus type 1 integrase (CHEMBL3471)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Azido-containing aryl beta-diketo acid HIV-1 integrase inhibitors.
Zhang X, Pais GC, Svarovskaia ES, Marchand C, Johnson AA, Karki RG, Nicklaus MC, Pathak VK, Pommier Y, Burke TR.
Bioorg Med Chem Lett (2003) 13 : 1215 -1219
PubMed 12643946 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.35 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20342 1 6.58
CHEMBL20091 1 5.82
CHEMBL20633 1 5.55
CHEMBL20586 1 5.21
CHEMBL20702 1 5.07
CHEMBL20117 1 4.62
CHEMBL20758 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20342 IC50 = 260.0 nM 6.58
CHEMBL20091 IC50 = 1500.0 nM 5.82
CHEMBL20633 IC50 = 2800.0 nM 5.55
CHEMBL20586 IC50 = 6100.0 nM 5.21
CHEMBL20702 IC50 = 8500.0 nM 5.07
CHEMBL20117 IC50 = 24000.0 nM 4.62
CHEMBL20758 IC50 = 25000.0 nM 4.60